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Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2Aserotoninreceptor, with an Ki of 397 nM .
Risperidone is a serotonin5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively.
DOI hydrochloride is a serotonin5-HT2A/2Creceptor agonist with Ki values of 0.7 nM, 2.4 nM and 20 nM for h5-HT2A,h5-HT2C and h5-HT2Breceptors, respectively. DOI hydrochloride can across the blood-brain barrier. DOI hydrochloride increases head twitches in mice .
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2Aserotoninreceptor, with an Ki of 397 nM .
Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A,5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na + channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation .
Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin5-HT1A receptor agonist and 5-HT2Areceptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research - .
Trimipramine maleate is a 5-HT receptor antagonist, with blood-brain barrier permeability. Trimipramine maleate has pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine maleate has vascular activity and anxiolytic efficacy .
Setiptiline (Org-8282) is a serotoninreceptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotoninreceptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
Bretisilocin (GM-2505) is the agonist for 5-HT2Areceptor and a serotonin releaser. Bretisilocin exhibits antidepressant activity and can be used in the study of depression .
Spiperone (Spiroperidol) is a potent dopamine D2, serotonin5-HT1A, and serotonin5-HT2A antagonist. Spiperone is also a labelled ligand for neuroleptic receptors. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. Spiperone has the potential for the research of neurology diseases .
Tegaserod is an orally active serotoninreceptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2Breceptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A,5-HT2B and 5-HT2Creceptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
Tegaserod maleate (SDZ-HTF-919) is an orally active serotoninreceptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2Breceptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A,5-HT2B and 5-HT2Creceptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotoninreceptors, showing a pEC50 of 8.90 at human D2receptors, a pEC50 of 8.09 at D3receptors, and a pEC50 of 6.28 at 5-HT1Areceptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1Areceptors, and suppresses serotonin-induced Ca 2+ release at 5-HT2Breceptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors . Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo .
Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin5-HT4receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2Breceptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease .
(R)-Fluoxetine hydrochloride, an antidepressant, is serotonin reuptake inhibitor (SSRI). (R)-Fluoxetine hydrochloride has modest affinity at the 5-HT2A and 5-HT2Creceptors .
Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole (HY-14546) and dopamine D2/D3receptor partial agonist. Dehydroaripiprazole also has certain affinity for serotonin5-HT1A, 5-HT2A and 5-HT2Breceptors. Dehydroaripiprazole has antipsychotic activity equivalent to Aripiprazole .
Glemanserin (MDL11939) is a potent and selective antagonist for serotoninreceptor5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively) .
Eplivanserin mixture (SR-46349 mixture) is a selective serotonin reuptake inhibitor and a 5-HT2Areceptor antagonist, extracted from patent WO 2005/002578 A1 .
Risperidone-d4 is the deuterium labeled Risperidone. Risperidone is a serotonin5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
α-Methylserotonin maleate is a potent and selective agonist of 5-HT2receptor. α-Methylserotonin maleate is an analogue of serotonin formed in vivo from α-Methyltryptophan. α-Methylserotonin maleate mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor-mediated phosphoinositide hydrolysis .
Kisspeptin 13 TFA is the TFA salt form of Kisspeptin 13 (HY-P3641). Kisspeptin-13 TFA inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 TFA activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 TFA interacts with α2-adrenergic and 5-HT2serotoninreceptors, exhibits antidepressant efficacy. Kisspeptin 13 TFA is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
IHCH-7113 (Compound 166) is an agonist of 5-HT2Aserotoninreceptor with antidepressant activity. IHCH-7113 is promising for research of antipsychotic agent .
Lurasidone metabolite 14326 is a minor active metabolite of Lurasidone (HY-B0032A) generated via metabolism by CYP3A4. Lurasidone metabolite 14326 shares similar receptor-binding properties with Lurasidone, acting as an antagonist of the dopamine D2 receptor (dopamine D2 receptor), an antagonist of the serotonin5-HT2A and 5-HT7 receptors(5-HT2A and 5-HT7 receptor), and a partial agonist of the serotonin 5-HT1A receptor. Lurasidone metabolite 14326 can be used in the research of schizophrenia and bipolar depression .
Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin5-HT4receptor (5-HT4R), with a pKi of 7.7. Velusetrag hydrochloride exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2Breceptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease .
VA012 (compound 11) is a positive allosteric modulator (PAM) of the serotonin5-HT2Creceptor. VA012 reduces food intake and body weight gain without causing CNS-related malaise during subchronic administration. VA012 can be utilized in obesity research .
Setiptiline maleate (MO-8282 maleate) is a serotoninreceptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotoninreceptor antagonist, likely at the 5-HT2A,5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
5-HT2A agonist 7 (Compound 45) is an orally active and highly selective serotoninreceptor 2A (5-HT2A) agonist (EC50=12 nM). 5-HT2A agonist 7 is promising for research of psychiatric disorders such as depression .
1-(Carboxymethyl)cyclohexanecarboxylic acid (1-Carboxycyclohexaneacetic acid; Gabapentin Impurity E) is a potential impurity in commercial preparations of the antiepileptic agent Gabapentin (HY-A0057). It is also used as a precursor for the synthesis of a serotonin (5-HT) receptor subtype 5-HT2A antagonist.
Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2Aserotoninreceptor, with an Ki of 397 nM .
Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2Aserotoninreceptor, with an Ki of 397 nM .
4-Hydroxy MET (4-HO-MET; 4-Hydroxy-N-methyl-N-ethyltryptamine) is a synthetic tryptamine psychoactive substance. 4-Hydroxy MET is a partial 5-HT2Areceptor agonist, a serotonin transporter inhibitor and weak norepinephrine transporter inhibitor. 4-Hydroxy MET affects emotional, motoric, and cognitive functions via serotonergic hallucinogenic activity .
Flibanserin (BIMT-17) hydrochloride (propan-2-ol) hydrate is an orally active serotonin5-HT1A receptor agonist and 5-HT2Areceptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin hydrochloride (propan-2-ol) hydrate binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin hydrochloride (propan-2-ol) hydrate shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research - .
Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .
Risperidone mesylate(R 64 766 mesylate) is a serotonin5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively.
5-HT2Areceptor agonist-2 is a highly potent serotonin5-HT2receptor agonists. 5-HT2Areceptor agonist-2 inspires 5-HT2A,5-HT2B, and 5-HT2C with EC50 values of 1.7, 0.58, and 0.50 nM, respectively .
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2serotoninreceptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
Iferanserin (S-MPEC) is a selective 5-HT receptor(serotoninreceptor) antagonist with an affinity for 5-HT2Areceptor. Iferanserin has the potential for internal hemorrhoid disease treatment .
Tedatioxetine (Lu AA24530) hydrobromide acts as a serotonin and norepinephrine (NE)-preferring triple reuptake inhibitor (TRI) and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist .
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RS130-180 is a selective β-arrestin-biased agonist targeting the serotonin 2A receptor(5-HT2aR). RS130-180 is promising for research of neuropsychiatric disorders such as depression .
Zicronapine is an antipsychotic agent with a strong pro-cognitive effect in animal models and the potential to treat a number of neurological and psychiatric diseases. Zicronapine has potent antagonistic effects at dopamine D1/D2, and serotonin5-HT2Areceptors .
Zicronapine (Lu 31-130) fumarate is an antipsychotic agent with a strong pro-cognitive effect in animal models and the potential to treat a number of neurological and psychiatric diseases. Zicronapine (Lu 31-130) fumarate has potent antagonistic effects at dopamine D1/D2, and serotonin5-HT2Areceptors .
LY53857 is a potent antagonist of vasoconstriction and serotonin-mediated 5-HT2receptors. LY53857 did not reduce mean arterial blood pressure in spontaneously hypertensive rats (SHR) at doses that blocked the depressor response to serotonin and blocked central serotoninreceptors. In addition, LY53857 was able to enhance neurotransmitter release in rat vas deferens and guinea pig ileal nerves .
CYB210010 is an orally bioavailable, long-acting serotonin5-HT2receptor agonist that selectively targets 5-HT2A and 5-HT2Creceptors (EC50: 4.1 n, 7.3 nM). CYB210010 can enter the central nervous system, cause a head twitch response (HTR), and is not prone to behavioral tolerance during chronic administration .
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively .
Metrenperone is an inhibitor for 5-HT2receptor. Metrenperone exhibits α1 and α2 antagonist activity as well as anti-H1 and anti-dopaminergic efficacy. Metrenperone can lower the blood pressure, enhances bradycardia in peripheral ischemia, inhibits serotonin-induced platelet aggregation, and antagonizes serotonin-mediated vasoconstriction. Metrenperone promotes the repair of acutely damaged collagen tissue .
Pruvanserin hydrochloride (EMD 281014) is a selective serotonin5-HT2Areceptor antagonist with IC50 values of 0.35 nM and 1 nM for human and rat 5-HT2Areceptors. Pruvanserin (hydrochloride) can be used for the research of schizophrenia .
Tedatioxetine (Lu AA24530) acts as a serotonin and norepinephrine (NE)-preferring triple reuptake inhibitor (TRI) and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist .
5-HT2Areceptor agonist-13 (Compound 28c) is a partial agonist of the 5-HT2Areceptor, with an EC50 value of 416.9 nM and a Ki value of 113.9 nM. 5-HT2Areceptor agonist-13 exhibits very weak agonistic activity towards the 5-HT2Breceptor (EC50 = 120.2 nM), D2 receptor (Ki = 1298 nM), and has no activity towards the 5-HT2Creceptor. 5-HT2Areceptor agonist-13 exhibits weak inhibitory activity on the serotonin transporter (SERT) (EC50 = 977.2 nM). 5-HT2Areceptor agonist-13 has antidepressant activity in mouse models and does not induce hallucinogenic behavior. 5-HT2Areceptor agonist-13 can be used for the study of major depressive disorder (MDD) and treatment-resistant depression (TRD) .
R-96544 (free base) is a potent, selective and competitive 5-HT2receptor antagonist. R-96544 (free base) inhibits platelet aggregation induced by serotonin, and inhibits 5-HT2Areceptor-mediated contraction of guinea pig trachea .
Trimipramine (Standard) is the analytical standard of Trimipramine. This product is intended for research and analytical applications. Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .
Trimipramine (maleate) (Standard) is the analytical standard of Trimipramine (maleate). This product is intended for research and analytical applications. Trimipramine maleate is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively . Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively . Trimipramine maleate has vascular activity and anxiolytic efficacy .
Risperidone E-oxime is an impurity of Risperidone . Risperidone is a serotonin5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
Risperidone (Standard) is the analytical standard of Risperidone. This product is intended for research and analytical applications. Risperidone is a serotonin5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively.
α-Methylserotonin is a potent and selective agonist of 5-HT2receptor. α-Methylserotonin is an analogue of serotonin formed in vivo from α-methyltryptophan. α-Methylserotonin mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor-mediated phosphoinositide hydrolysis .
Risperidone-d4-1 (R 64 766-d4-1) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively.
Risperidone E-oxime (Standard) is the analytical standard of Risperidone E-oxime. This product is intended for research and analytical applications. Risperidone E-oxime is an impurity of Risperidone . Risperidone is a serotonin5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
Etoperidone, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone shows Kd values of 36 nM, 38 nM, 85 nM, and 570 nM for 5-HT2receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively .
Etoperidone hydrochloride, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone hydrochloride shows Kd values of 36 nM, 38 nM, 85 nM, and 570 nM for 5-HT2receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively .
ICI 169369 is an orally active, specific serotonin and 5-HT2/5-HT1Creceptor competitive antagonist. ICI 169369 exhibits Ki values of 1.79 x 10 −8 and 1.58 x 10 −6 M for 5-HT2 and 5-HT1, respectively .
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2Aserotoninreceptor, with an Ki of 397 nM .
Trimipramine (Standard) is the analytical standard of Trimipramine. This product is intended for research and analytical applications. Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .
Setiptiline-d3 is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotoninreceptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotoninreceptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
Setiptiline (Standard) is the analytical standard of Setiptiline. This product is intended for research and analytical applications. Setiptiline (Org-8282) is a serotoninreceptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotoninreceptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
Setiptiline (maleate) (Standard) is the analytical standard of Setiptiline (maleate). This product is intended for research and analytical applications. Setiptiline maleate (MO-8282 maleate) is a serotoninreceptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotoninreceptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
Glemanserin (Standard) is the analytical standard of Glemanserin. This product is intended for research and analytical applications. Glemanserin (MDL11939) is a potent and selective antagonist for serotoninreceptor5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively) .
MRS8209 is the antagonist for serotoninreceptor with a Ki of 4.27 nM for 5-HT2BR. MRS8209 exhibits protective effect on pressure at airway opening (PAO), and can be used in research of pulmonary fibrosis .
25N-NBOMe hydrochloride, a 2C-N derivative, is a 5-HT2A and 5-HT2Creceptors agonist with Ki values of 0.144 nM and 1.06 nM, respectively. 25N-NBOMe hydrochloride has little to no efficacy at inducing release of preloaded neurotransmitter from recombinant dopamine, serotonin and norepinephrine transporters .
Flibanserin-d4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM) .
Metergoline (Standard) is the analytical standard of Metergoline. This product is intended for research and analytical applications. Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na+ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation .
ECPLA, a lysergamide lysergic acid diethylamidean (LSD) analog, is a potent 5-HT2A agonist (EC50 of 14.6 nM) for Gq-mediated calcium flux. ECPLA has high affinity for most serotoninreceptors, α2-adrenoceptors, and D2-like dopamine receptors .
Tegaserod-d11 is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotoninreceptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2Breceptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A,5-HT2B and 5-HT2Creceptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
Dehydroaripiprazole (Standard) is the analytical standard of Dehydroaripiprazole. This product is intended for research and analytical applications. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole (HY-14546) and dopamine D2/D3receptor partial agonist. Dehydroaripiprazole also has certain affinity for serotonin5-HT1A, 5-HT2A and 5-HT2Breceptors. Dehydroaripiprazole has antipsychotic activity equivalent to Aripiprazole .
Spiperone (Standard) is the analytical standard of Spiperone. This product is intended for research and analytical applications. Spiperone (Spiroperidol) is a potent dopamine D2, serotonin 5-HT1A, and serotonin5-HT2A antagonist. Spiperone is also a labelled ligand for neuroleptic receptors. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. Spiperone has the potential for the research of neurology diseases .
Centpropazine (CNPZ) is a brain-penetrant and non-selective antagonist of serotonin(5-HT1/5-HT2) and adrenergic (α1) receptors. Centpropazine functions by modulating monoamine neurotransmission, particularly reducing serotonin and norepinephrine reuptake, to exert antidepressant effects. Centpropazine is promising for research of depression .
Flibanserin-d4-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD) .
Brilaroxazine (Standard) is the analytical standard of Brilaroxazine. This product is intended for research and analytical applications. Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors . Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo .
Flibanserin (Standard) is the analytical standard of Flibanserin. This product is intended for research and analytical applications. Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin5-HT1A receptor agonist and 5-HT2Areceptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research - .
1-(Carboxymethyl)cyclohexanecarboxylic acid (Standard) is the analytical standard of 1-(Carboxymethyl)cyclohexanecarboxylic acid. This product is intended for research and analytical applications. 1-(Carboxymethyl)cyclohexanecarboxylic acid (1-Carboxycyclohexaneacetic acid; Gabapentin Impurity E) is a potential impurity in commercial preparations of the antiepileptic agent Gabapentin (HY-A0057). It is also used as a precursor for the synthesis of a serotonin (5-HT) receptor subtype 5-HT2A antagonist.
1-(Carboxymethyl)cyclohexanecarboxylic acid (Standard) is the analytical standard of 1-(Carboxymethyl)cyclohexanecarboxylic acid. This product is intended for research and analytical applications. 1-(Carboxymethyl)cyclohexanecarboxylic acid (1-Carboxycyclohexaneacetic acid; Gabapentin Impurity E) is a potential impurity in commercial preparations of the antiepileptic agent Gabapentin (HY-A0057). It is also used as a precursor for the synthesis of a serotonin (5-HT) receptor subtype 5-HT2A antagonist.
BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotoninreceptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2Areceptors, respectively. BL-1020 mesylate is agonist for GABAAreceptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate .
Platelet aggregation-IN-3 (Compound 5) is a ligand for H2 histamine receptors, α2(A,C)-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotoninreceptors. Platelet aggregation-IN-3 can inhibit platelet aggregation induced by ADP and collagen and can also modulate tumour cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 is promising for research of antiplatelet therapy in cardiovascular diseases and the prevention of cancer-related thrombosis and tumour metastasis .
7-Hydroxyrisperidone (7-RispOH) is a metabolite of Risperidone (HY-11018). Risperidone is a serotonin5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist .
5-HT2A antagonist 4 methanesulfonate (Example 29) is a dopamine D2 receptor and serotonin5HT2A receptor antagonist. 5-HT2A antagonist 4 methanesulfonate can be used for the study of central nervous system diseases .
TCB2 (Standard) is the analytical standard of TCB2 (HY-103102). This product is intended for research and analytical applications. TCB2 is an agonist of serotonin5-HT2Areceptor.
DOI hydrochloride (Standard) is the analytical standard of DOI hydrochloride (HY-103124). This product is intended for research and analytical applications. DOI hydrochloride is a serotonin5-HT2A/2Creceptor agonist with Ki values of 0.7 nM, 2.4 nM and 20 nM for h5-HT2A, h5-HT2C and h5-HT2Breceptors, respectively. DOI hydrochloride can across the blood-brain barrier. DOI hydrochloride increases head twitches in mice .
AT-1015 is a selective and orally active 5-HT2Aserotoninreceptor antagonist. AT-1015 exhibits antithrombotic effect. AT-1015 prolongs the time needed to occlusion of the artery with thrombus. AT-1015 impairs platelet aggregation and vasoconstriction .
Tedatioxetine hydrobromide (Standard) (Lu AA24530 hydrobromide (Standard)) is the analytical standard of Tedatioxetine hydrobromide (HY-101755). This product is intended for research and analytical applications. Tedatioxetine (Lu AA24530) hydrobromide acts as a serotonin and norepinephrine (NE)-preferring triple reuptake inhibitor (TRI) and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist .
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Velusetrag hydrochloride (Standard) is the analytical standard of Velusetrag hydrochloride (HY-10457A). This product is intended for research and analytical applications. Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag hydrochloride exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2Breceptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease .
Velusetrag (Standard) is the analytical standard of Velusetrag (HY-10457). This product is intended for research and analytical applications. Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2Breceptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease .
Desmethyl cariprazine-d8 is the deuterium labeled Desmethyl cariprazine (HY-100656). Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotoninreceptors, showing a pEC50 of 8.90 at human D2 receptors, a pEC50 of 8.09 at D3 receptors, and a pEC50 of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca 2+ release at 5-HT2Breceptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
Clozapine (HF 1854) dihydrochloride is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Clozapine hydrochloride (HF 1854 hydrochloride) is an antipsychotic used for the research of schizophrenia. Clozapine hydrochloride has high affinity for a number of neuroreceptors. Clozapine hydrochloride is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and serotonin5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine hydrochloride is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Olanzapine hydrochloride is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine hydrochloride is an atypical antipsychotic .
Piromelatine (Standard) is the analytical standard of Piromelatine. This product is intended for research and analytical applications. Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities .
Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Clozapine (Standard) is the analytical standard of Clozapine. This product is intended for research and analytical applications. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Olanzapine-d3 (LY170053-d3) is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotoninreceptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain .
Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotoninreceptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain .
Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptorP2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotoninreceptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7 .
Opiranserin hydrochloride (Standard) is the analytical standard of Opiranserin (hydrochloride) (HY-109067A). This product is intended for research and analytical applications. Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotoninreceptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain .
SCH 50911 is a selective, orally active, blood-brain barrier permeable GABA-B receptor (GABA-B Receptor) antagonist with an IC50 of 1.1 μM in rats. SCH 50911 blocks baclofen-induced antitussive effects, regulates neuronal firing and GABA release. SCH 50911 promotes spontaneous seizures during withdrawal in ethanol-dependent rats, alters reward-related neurotransmission, and reduces or suppresses lever responding and self-administration behaviors of alcohol and sucrose in rats. SCH 50911 is applicable to research related to ethanol withdrawal syndrome, absence epilepsy and alcohol use disorder .
Mosapramine (Clospipramine) is an orally active antipsychotic agent and one of the metabolites of Clocapramine (HY-B2073) after oral absorption. Mosapramine exerts its effects by specifically binding to striatal dopamine D2 receptors and frontal lobe 5-HT2 receptors, with a D2/5-HT2 receptor occupancy ratio of 7.4. Mosapramine induces typical neuropharmacological responses in rat brain regions, including extrapyramidal symptoms, hyperprolactinemia, increased salivation, constipation, and upregulated Fos protein expression. Mosapramine also features a reduced incidence of weight loss. Mosapramine is applicable to research related to schizophrenia .
Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2Aserotoninreceptor, with an Ki of 397 nM .
α-Methylserotonin maleate is a potent and selective agonist of 5-HT2receptor. α-Methylserotonin maleate is an analogue of serotonin formed in vivo from α-Methyltryptophan. α-Methylserotonin maleate mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor-mediated phosphoinositide hydrolysis .
Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2Aserotoninreceptor, with an Ki of 397 nM .
Kisspeptin 13 TFA is the TFA salt form of Kisspeptin 13 (HY-P3641). Kisspeptin-13 TFA inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 TFA activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 TFA interacts with α2-adrenergic and 5-HT2serotoninreceptors, exhibits antidepressant efficacy. Kisspeptin 13 TFA is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2serotoninreceptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2Aserotoninreceptor, with an Ki of 397 nM .
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2Aserotoninreceptor, with an Ki of 397 nM .
Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2Aserotoninreceptor, with an Ki of 397 nM .
Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2Aserotoninreceptor, with an Ki of 397 nM .
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2Aserotoninreceptor, with an Ki of 397 nM .
Trimipramine (Standard) is the analytical standard of Trimipramine. This product is intended for research and analytical applications. Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .
5HT2A Protein, Human (S162K, M164W, sf9, Flag, His) is the recombinant human-derived 5HT2A, expressed by sf9 insect cells, with His, Flag labeled tag.,
5HT2A Protein, Human (L247A, L371A, sf9, Flag, His) is the recombinant human-derived 5HT2A, expressed by sf9 insect cells, with His, Flag labeled tag.,
Risperidone-d4 is the deuterium labeled Risperidone. Risperidone is a serotonin5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
Olanzapine-d3 (LY170053-d3) is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively .
Risperidone-d4-1 (R 64 766-d4-1) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin5-HT2receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2receptor, respectively.
Setiptiline-d3 is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotoninreceptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotoninreceptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
Flibanserin-d4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM) .
Tegaserod-d11 is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotoninreceptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2Breceptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A,5-HT2B and 5-HT2Creceptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
Flibanserin-d4-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD) .
Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Desmethyl cariprazine-d8 is the deuterium labeled Desmethyl cariprazine (HY-100656). Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotoninreceptors, showing a pEC50 of 8.90 at human D2 receptors, a pEC50 of 8.09 at D3 receptors, and a pEC50 of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca 2+ release at 5-HT2Breceptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
RS130-180 is a selective β-arrestin-biased agonist targeting the serotonin 2A receptor(5-HT2aR). RS130-180 is promising for research of neuropsychiatric disorders such as depression .
Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2Aserotoninreceptor, with an Ki of 397 nM .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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