5-HT Receptor Inhibitor

PZ-1657 hydrochloride (Compound 57) is a potent, selective and orally active 5-HT7 receptor inverse agonist with a K_i of 5 nM. PZ-1657 hydrochloride can inhibit the constitutive cAMP production mediated by the Gs signaling pathway (EC₅₀ = 2.93 nM). PZ-1657 hydrochloride can significantly reduce the MMP-9 activity mediated by 5-HT7 receptors in the hippocampus of mice, and the effect is comparable to that of SB-269970 (HY-15370). PZ-1657 hydrochloride can reverse the cognitive deficits observed in the rat novel object recognition test induced by Phencyclidine without affecting the animals' spontaneous activities. PZ-1657 hydrochloride can be used for the research of emotional disorders, such as depression and bipolar disorder.

Melitracen (Melitracene) is an orally active tricyclic antidepressant and it is also a bipolar thymoleptic with activating properties. Melitracen inhibits ³H-5-HT and ¹⁴H-5-HT with IC₅₀s of 670 nM and 5500 nM, respectively. Melitracen can be used for the research of depression and anxiety.

Pimavanserin-d₄ (ACP-103-d₄) is the deuterium labeled Pimavanserin (HY-14557). Pimavanserin is a selective, brain-penetrant, inverse agonist of the 5-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively.

Belaperidone (LU-111995), a 5-HT_2A receptor inhibitor, possesses antidopaminergic and antiserotonergic effects.

Lofepramine (Lopramine) is a modified tricyclic and orally active antidepressant. Lofepramine inhibits the uptake of Noradrenaline (NA) (HY-13715) and 5-hydroxytryptamine (5-HT) with IC₅₀s of 2.7 μM and 11 μM, respectively. Lofepramine exerts its antidepressant activity by promoting noradrenergic neurotransmission. Lofepramine also enhances serotonergic neurotransmission by inhibiting neuronal uptake of 5-HT and tryptophan pyrrolase. Lofepramine exhibits significant anxiolytic properties. .

(R)-Citalopram oxalate (Standard) is the analytical standard of (R)-Citalopram oxalate. This product is intended for research and analytical applications. (R)-Citalopram oxalate, a R-(-) enantiomers of Citalopram (HY-121203), is a serotonin reuptake inhibitor. (R)-Citalopram oxalate is at least 20-fold weaker than S-citalopram (HY-14258) as inhibitor of the 5-HT transporter (SERT). (R)-Citalopram oxalate can be used for research of depression.

Napamezole is an orally active α-2 adrenergic receptor antagonist and serotonin (5-HT Receptor) reuptake inhibitor, with K_i values of 28 nM and 93 nM for rat α-2 and α-1 adrenergic receptors, respectively. Napamezole can be used for the research of depression.

LY125180 is a serotonin uptake inhibitor. LY125180 competitively inhibits the uptake of serotonin and norepinephrine by cortical synaptosomes and of dopamine by striatal synaptosomes, with K_i values of 0.06 μM, 2.2 μM and 2.5 μM respectively.

Cyproheptadine hydrochloride (Standard) (Cyproheptadine HCl (Standard)) is the analytical standard of Cyproheptadine hydrochloride (HY-B0366A). This product is intended for research and analytical applications. Cyproheptadine hydrochloride (Cyproheptadine HCl) acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.

LY2624803 is a 5-HT2A and histamine, H1 receptor antagonist.

BMS-570520 is an orally bioavailable CCR3 antagonist with an IC₅₀ of 1.9 nM against hCCR3 and an IC₅₀ of 1300 nM against hCYP2D6. BMS-570520 inhibits CYP2D6, but shows low activity against off-target G protein-coupled receptors, biogenic amine transporters, and the hERG potassium channel. BMS-570520 regulates chemotaxis, calcium mobilization, and anti-inflammatory pathways. BMS-570520 can be used in research related to asthma, allergic rhinitis, and contact dermatitis.

Fezolamine is an orally active non-tricyclic compound , and shows antidepressant activity.

S 32212 hydrochloride is an inverse agonist of 5-HT receptors 5-HT2(CINI) and 5-HT2(CVSV) (Kis=6.6, 8.9 nM) and an antagonist of 5-HT2A and α2β-adrenergic receptors (Ki=5.8, 5.8 nM). S 32212 hydrochloride can reduce the binding of GTPγS to Gαq, and reduce the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2(CINI) receptor and CHO cells expressing 5-HT2(CVSV) receptor (EC₅₀=38 and 18.6 nM, respectively). S 32212 hydrochloride (2.5 mg/kg) reduces 5-HT receptor agonist-induced head twitches and penile erections in mice and rats. S 32212 hydrochloride (10, 40 mg/kg) reduces immobility time in the forced swim test and marble burying behavior in mice and rats, exerting antidepressant and anxiolytic activities.

Risperidone (Standard) is the analytical standard of Risperidone. This product is intended for research and analytical applications. Risperidone is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

LY 178210 (Compound 24) is a selective partial agonist of the 5-HT1A receptor, with K_i values ​​of 0.67 and 380 nM for the 5-HT1A and 5-HT1D receptors, respectively. LY 178210 has almost no activity against α₂-adrenergic receptors, 5-HT₂, and other neurotransmitter receptors. LY 178210 inhibits Foscolin-stimulated cyclase activity, but its maximum potency is lower than that of the full agonist 8-OH-DPAT (HY-112061). LY 178210 significantly reduces 5-hydroxyindoleacetic acid (5-HIAA) levels in the greater hypothalamus and increases serum corticosterone concentrations.

Litoxetine (SL 81.0385) is a selective 5-HT uptake inhibitor. Litoxetine is a 5-HT₃ receptor antagonist with a K_i of 85 nM for cerebral 5-HT₃ receptors. Litoxetine is an antidepressant and has antiemetic properties.

Paroxetine-d₂ (BRL29060-d₂) is the deuterated-labeled Paroxetine (HY-122272). Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.

Risperidone-d4-1 (R 64 766-d4-1) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

AChE-IN-5 (compound 5) exhibits strong in vitro bioactivity against AChE/5-HT_1A/SERT and exhibits good BBB permeability. AChE-IN-5 shows IC₅₀ value 2.29 nM against AChE, EC₅₀ value 58.6 nM against 5-HT_1A and IC₅₀ value against SERT. Orally active.

5-Bromo-N,N-dimethyltryptamine, an active metabolite, is an antidepressant and sedative drug lead. 5-Bromo-N,N-dimethyltryptamine shows strong affinity towards 5-HT_1A, 5-HT_2B, 5-HT₆, and 5-HT₇.