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Results for "

5-HT releasers

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (50) Adrenergic Receptor (2) Apoptosis (2) Calcium Channel (2) Caspase (2) Dopamine Receptor (7) Dopamine Transporter (5) Drug Derivative (2) Drug Metabolite (1) Endogenous Metabolite (1) Epigenetic Reader Domain (2) ERK (2) FAAH (1) FGFR (2) Fluorescent Dye (1) GABA Receptor (1) Histamine Receptor (2) Interleukin Related (1) Isotope-Labeled Compounds (5) Lactate Dehydrogenase (1) Monoamine Transporter (1) nAChR (2) Neurokinin Receptor (3) Opioid Receptor (1) p38 MAPK (2) Phosphodiesterase (PDE) (2) Potassium Channel (2) Reference Standards (1) Serotonin Transporter (6) Syk (4) TGF-β Receptor (2) Tyrosine Hydroxylase (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (6) Inflammation/Immunology (5) Metabolic Disease (8) Neurological Disease (50)

By Targets:

5-HT Receptor (50)

Adrenergic Receptor (2)

Apoptosis (2)

Calcium Channel (2)

Caspase (2)

Dopamine Receptor (7)

Dopamine Transporter (5)

Drug Derivative (2)

Drug Metabolite (1)

Endogenous Metabolite (1)

Epigenetic Reader Domain (2)

ERK (2)

FAAH (1)

FGFR (2)

Fluorescent Dye (1)

GABA Receptor (1)

Histamine Receptor (2)

Interleukin Related (1)

Isotope-Labeled Compounds (5)

Lactate Dehydrogenase (1)

Monoamine Transporter (1)

nAChR (2)

Neurokinin Receptor (3)

Opioid Receptor (1)

p38 MAPK (2)

Phosphodiesterase (PDE) (2)

Potassium Channel (2)

Reference Standards (1)

Serotonin Transporter (6)

Syk (4)

TGF-β Receptor (2)

Tyrosine Hydroxylase (1)

By Research Areas:

Cancer (2)

Cardiovascular Disease (6)

Inflammation/Immunology (5)

Metabolic Disease (8)

Neurological Disease (50)

Inhibitors & Agonists

Fluorescent Dyes

Peptides

Isotope-Labeled Compounds

Targets Recommended: 5-HT Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13409

SB 242084 Maximum Cited Publications 6 Publications Verification	5-HT Receptor	Neurological Disease Metabolic Disease
SB 242084 is a selective, competitive and high-affinity (pK_i=9.0) 5-HT_2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT_2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage .

HY-172420

Bretisilocin GM-2505	5-HT Receptor	Neurological Disease
Bretisilocin (GM-2505) is the agonist for 5-HT_2A receptor and a serotonin releaser. Bretisilocin exhibits antidepressant activity and can be used in the study of depression .

HY-B0383

Almotriptan malate PNU180638	5-HT Receptor	Neurological Disease
Almotriptan malate (PNU180638) is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine .

HY-100656

Desmethyl cariprazine	Dopamine Receptor 5-HT Receptor	Neurological Disease
Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, 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-HT_1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT_1A receptors, and suppresses serotonin-induced Ca ²⁺ release at 5-HT_2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.

HY-P1422

Spadin 1 Publications Verification	Potassium Channel 5-HT Receptor	Neurological Disease
Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC₅₀ value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research .

HY-13409A

SB 242084 dihydrochloride Maximum Cited Publications 6 Publications Verification	5-HT Receptor	Neurological Disease Metabolic Disease
SB 242084 dihydrochloride is a selective, competitive and high-affinity (pK_i=9.0) 5-HT_2C receptor antagonist (crosses the blood-brain barrier). SB 242084 dihydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 dihydrochloride also increases mitochondrial gene expression and oxidative metabolism via 5-HT_2A receptor. SB 242084 dihydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage .

HY-15472

PRX-08066	5-HT Receptor p38 MAPK TGF-β Receptor FGFR Apoptosis Caspase	Cardiovascular Disease Neurological Disease Cancer
PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a K_i of 3.4 nM. PRX-08066 inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 inhibits pulmonary vascular remodeling. PRX-08066 can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET) .

HY-B0383A

Almotriptan PNU180638 free base	5-HT Receptor	Neurological Disease
Almotriptan (PNU180638 free base) is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan can be used in research related to migraine .

HY-12143

Vofopitant dihydrochloride GR 205171A	Neurokinin Receptor	Neurological Disease
Vofopitant dihydrochloride (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant dihydrochloride blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant dihydrochloride exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant dihydrochloride improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant dihydrochloride can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .

HY-D2335

SERTlight	Fluorescent Dye	Neurological Disease
SERTlight is a fluorescent agent that can specifically label serotonergic neuronal cell bodies, dendrites, and axonal projections as fluorescent substrates of the serotonin transporter (SERT). SERTlight is orthogonal to various genetically encoded sensors in terms of optics, pharmacology, and operation, enabling multiple imaging. SERTlight allows the use of GRAB_5HT sensors to label distal 5HT axonal projections and simultaneously image the release of endogenous 5HT, providing a new multifunctional molecular tool for studying serotonergic systems .

HY-112390A

Syk Inhibitor II 2 Publications Verification	Syk 5-HT Receptor	Inflammation/Immunology
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC₅₀ of 41 nM. Syk Inhibitor II inhibits *5-HT* release from RBL-cells with an IC₅₀ of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect .

HY-106865

Mivazerol	Dopamine Receptor Adrenergic Receptor	Cardiovascular Disease
Mivazerol is a selective α2-adrenoceptor agonist. Mivazerol decreases the spontaneous release of serotonin (5-HT) and significantly inhibits the immobilization stress-induced enhancement of norepinephrine (NE), dopamine (DA) and dihydroxyphenylacetic acid (DOPAC). Mivazerol inhibits intrathecal release of glutamate evoked by halothane withdrawal in rats, and exerts neuroprotective effects in forebrain ischemia rats. Mivazerol can be used for myocardial ischemia research _.

HY-129101

(-)-Eseroline fumarate Eseroline fumarate	5-HT Receptor	Neurological Disease
(-)-Eseroline fumarate is a metabolic of Physostigmine (HY-N6608), an AChE inhibitor. (-)-Eseroline fumarate elicits a leakage of lactic acid dehydrogenase (LDH) from cancer cells. (-)-Eseroline fumarate also induces the release of adenine nucleotides and 5-hydroxytryptamine (5-HT) from neuronal cells, thus induce cell death. (-)-Eseroline fumarate inhibits the electrically evoked twitches of the mouse vas deferens and of the guinea-pig ileum .

HY-19026

Siguazodan SKF 94836	Phosphodiesterase (PDE)	Cardiovascular Disease
Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC₅₀ of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC₅₀ of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC₅₀ value of 4.2 μM .

HY-P1422A

Spadin TFA 1 Publications Verification	Potassium Channel 5-HT Receptor	Neurological Disease
Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC₅₀ value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research .

HY-19283

DU125530	5-HT Receptor	Neurological Disease
DU125530 is a potent and selective5-HT1A receptor antagonist with K_i values of 0.7, 890, 1200, 240, 750, 1100 nM for 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2C, 5-HT3, respectively. DU125530 shows antidepressant effects .

HY-124086

BHQ-O-5HT	5-HT Receptor	Neurological Disease
BHQ-O-5HT is a light-activated caged 5-HT protected by a BHQ group. When exposed to light at 365 or 740 nm, BHQ-O-5HT releases 5-HT through 1 or 2 photon excitation, respectively. BHQ-O-5HT can be manipulated in space and time to explore the role of 5-HT in regulating mood, appetite, memory, learning, and other cognitive functions .

HY-W707158

Norfenfluramine hydrochloride (±)-Norfenfluramine hydrochloride	Drug Metabolite Serotonin Transporter	Neurological Disease
Norfenfluramine hydrochloride ((±)-Norfenfluramine hydrochloride) is a major and brain-penetrant metabolite of Fenfluramine. Norfenfluramine hydrochloride can interact with 5-HT transporters to release 5-HT from neurons. Norfenfluramine hydrochloride displays antiepileptic effects in vivo .

HY-12142

Vofopitant GR 205171	Neurokinin Receptor	Neurological Disease
Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .

HY-175515

5-HT2C agonist-11	5-HT Receptor	Neurological Disease
5-HT2C agonist-11 (Compound 1) is an orally active, brain-penetrant and selective 5-HT_2C receptor agonist (EC₅₀=15 nM). 5-HT2C agonist-11 activates the Gq protein signaling pathway, promoting intracellular calcium release. 5-HT2C agonist-11 is promising for research of depression, post-traumatic stress disorder (PTSD) and neuropathic pain .

HY-19742A

Lecozotan hydrochloride SRA-333 hydrochloride	5-HT Receptor	Neurological Disease
Lecozotan (SRA-333) hydrochloride is an orally active and selective antagonist of *5-HT_1A* with a K_i of 4.5 nM for cloned human 5-HT_1A receptor. Lecozotan hydrochloride enhances the stimulated release of glutamate and acetylcholine in the hippocampus and possesses cognitive-enhancing properties. Lecozotan hydrochloride has the potential for mild-to-moderate Alzheimer's disease (AD) research .

HY-101377A

R(+)-8-OH-DPAT hydrobromide (R)-8-Hydroxy-2-dipropylaminotetralin hydrobromide	5-HT Receptor	Neurological Disease
R(+)-8-OH-DPAT ((R)-8-Hydroxy-2-dipropylaminotetralin) hydrobromide is a potent *5-HT_1A* agonist. R(+)-8-OH-DPAT potentiates SUL (HY-B1059)-induced dopamine (DA) release in the medial prefrontal cortex (mPFC) .

HY-P3839

Nocistatin	Opioid Receptor	Neurological Disease
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a G_i/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .

HY-156807

LY 367265	Serotonin Transporter 5-HT Receptor	Neurological Disease
LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder .

HY-137162

Dotarizine	Drug Derivative Calcium Channel Lactate Dehydrogenase 5-HT Receptor	Neurological Disease
Dotarizine is a novel Piperazine (HY-B0912) derivative and antimigraine agent. Dotarizine exhibits Ca ²⁺ channel blocking properties. Dotarizine decreases the release of lactate dehydrogenase. Dotarizine shows 5-HT receptor blocking effect .

HY-W681014

5-Fluoro-α-methyltryptamine hydrochloride	5-HT Receptor Dopamine Receptor	Neurological Disease
5-Fluoro-α-methyltryptamine hydrochloride may cause an increase in intracellular levels of 5-HT followed by an increase in 5-HT release. 5-Fluoro-α-methyltryptamine hydrochloride exhibits EC₅₀ values of 37 nM, 14 nM, 78 nM and 8.47 nM for DA, *5HT, NE and 5-HT2A*, respectively .

HY-112390

Syk Inhibitor II dihydrochloride	5-HT Receptor Syk	Inflammation/Immunology
Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC₅₀ of 41 nM. Syk Inhibitor II dihydrochloride inhibits *5-HT* release from RBL-cells with an IC₅₀ of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect .

HY-14149A

Cisapride monohydrate 2 Publications Verification R 51619 monohydrate; (±)-Cisaprid monohydrate	5-HT Receptor	Neurological Disease Metabolic Disease
Cisapride monohydrate is an orally and potent *5-HT₄* receptor agonist and hERG inhibitor. Cisapride monohydrate is an prokinetic agent which facilitates or restores motility throughout the length of the gastrointestinal tract. Cisapride monohydrate stimulates gastrointestinal motor activity through an indirect mechanism involving the release of acetylcholine mediated by postganglionic nerve endings in the myenteric plexus of the gut .

HY-116680

LY53857	5-HT Receptor	Cardiovascular Disease Neurological Disease
LY53857 is a potent antagonist of vasoconstriction and serotonin-mediated *5-HT₂* receptors. 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 serotonin receptors. In addition, LY53857 was able to enhance neurotransmitter release in rat vas deferens and guinea pig ileal nerves .

HY-W018475

Rizatriptan MK 462 free base	5-HT Receptor	Neurological Disease
Rizatriptan (MK 462 free base) is an orally active 5-HT_1B/5-HT_1D receptor agonist, with BBB permeability. Rizatriptan exerts significant anti-migraine effects by constricting intracranial and extracranial blood vessels and inhibiting neuropeptide release. Rizatriptan exhibits species- and tissue-specific metabolic characteristics; for example, it undergoes oxidative deamination mainly by MAO-A in the liver of brown rats, so co-administration with MAO-A inhibitors is prohibited. Rizatriptan may also exacerbate nitroglycerin-induced cutaneous allodynia, prolong the duration of central sensitization, and increase anxiety-like behavior and active drug-seeking behavior in mice. Rizatriptan has been widely used in studies related to migraine and medication-overuse headache .

HY-127023

Eicosapentaenoyl serotonin EPA-5-HT	Endogenous Metabolite FAAH Interleukin Related Tyrosine Hydroxylase	Metabolic Disease
Eicosapentaenoyl serotonin (EPA-5-HT) is an endogenous fatty acid-serotonin conjugate lipid mediator. Eicosapentaenoyl serotonin acts as an inhibitor of fatty acid amide hydrolase (FAAH). Eicosapentaenoyl serotonin suppresses IL-17 release in Concanavalin A (HY-P2149)-stimulated human peripheral blood mononuclear cells. Eicosapentaenoyl serotonin is regulated by polyunsaturated fatty acids and modulates intestinal immunity and Th17 signaling. Eicosapentaenoyl serotonin can be used for the study of inflammatory bowel disease-related mechanisms .

HY-59201A

A-582941 dihydrochloride	ERK 5-HT Receptor Epigenetic Reader Domain nAChR	Neurological Disease Metabolic Disease
A-582941 dihydrochloride is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with K_i values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 dihydrochloride exhibits agonistic activity at *5-HT3* receptors, with a K_i of 150 nM. A-582941 dihydrochloride triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 dihydrochloride is applicable for the research of Alzheimer's disease and schizophrenia .

HY-W728110

5-MeO-pyr-T 5-Methoxy pyrrolidinyltryptamine	5-HT Receptor	Neurological Disease
5-MeO-pyr-T (5-Methoxy pyrrolidinyltryptamine) is a *5-HT1AR* agonist, with K_is of 0.577 and 373 μM for 5-HT1AR and 5-HT2AR respectively. 5-MeO-pyr-T inhibits 5-HT uptake and elicits 5-HT release. 5-MeO-pyr-T induces hypolocomotion .

HY-169467

5-Chloro-α-methyltryptamine	5-HT Receptor Dopamine Receptor	Neurological Disease
5-Chloro-α-methyltryptamine (Compound 7b) is a potent and selective dual *DA/5-HT* releaser and *5-HT_2a* agonist. 5-Chloro-α-methyltryptamine releases DA and *5-HT* with the EC₅₀ values of 54.3 nM and 16.2 nM, respectively. 5-Chloro-α-methyltryptamine can be used in the study of neurotransmitter .

HY-19846

VRX-03011 PRX-03140 potassium salt	5-HT Receptor	Others
VRX-03011 (PRX-03140 (potassium salt)) is a compound with the potential to enhance memory and regulate acetylcholine release. It is a 5-HT? agonist that can enhance memory, regulate hippocampal acetylcholine efflux, and regulate APP metabolism without gastrointestinal side effects.

HY-162511

IP2015	Dopamine Transporter Serotonin Transporter	Others
IP2015 is an inhibitor for monoamine reuptake, that inhibits the reuptake of dopamine, serotonin (5-HT), and noradrenaline. IP2015 increases release of central dopamine and peripheral nitric oxide (NO), causes the NO-mediated relaxation of erectile tissue, and thus induces erection in rat model .

HY-112390C

Syk Inhibitor II hydrochloride	5-HT Receptor Syk	Inflammation/Immunology
Syk Inhibitor II hydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC₅₀ of 41 nM. Syk Inhibitor II hydrochloride inhibits *5-HT* release from RBL-cells with an IC₅₀ of 460 nM. Syk Inhibitor II hydrochloride shows less potent against other kinases and has anti-allergic effect .

HY-112390B

Syk Inhibitor II dihydrochloride dihydrate	Syk 5-HT Receptor	Inflammation/Immunology
Syk Inhibitor II dihydrochloride dihydrate is a potent, high selective and ATP-competitive Syk inhibitor with an IC₅₀ of 41 nM. Syk Inhibitor II dihydrochloride dihydrate inhibits *5-HT* release from RBL-cells with an IC₅₀ of 460 nM. Syk Inhibitor II dihydrochloride dihydrate shows less potent against other kinases and has anti-allergic effect .

HY-12142S

rac-Vofopitant-d3 rac-GR 205171-d₃	Isotope-Labeled Compounds Neurokinin Receptor	Neurological Disease
rac-Vofopitant-d₃ (rac-GR 205171-d₃) is a racemic form of deuterated Vofopitant (HY-12142). Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .

HY-W061043

DOV-216,303	Serotonin Transporter Dopamine Transporter	Neurological Disease
DOV-216,303 is an antidepressant compound. DOV-216,303 inhibits the reuptake of norepinephrine (NE), serotonin (5‐HT), and dopamine (DA), with IC₅₀ values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively. DOV-216,303 increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats .

HY-19026R

Siguazodan (Standard) SKF 94836 (Standard)	Phosphodiesterase (PDE) Reference Standards	Cardiovascular Disease
Siguazodan (Standard) is the analytical standard of Siguazodan. This product is intended for research and analytical applications. Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM .

HY-15472A

PRX-08066 maleate	5-HT Receptor p38 MAPK TGF-β Receptor FGFR Apoptosis Caspase	Cardiovascular Disease Neurological Disease Cancer
PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a K_i of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET) .

HY-111136

BL-1020 mesylate	GABA Receptor 5-HT Receptor Dopamine Receptor Histamine Receptor	Neurological Disease
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 serotonin receptor (5-HT receptor), with K_i of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABA_A receptor with K_i of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (K_i is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate .

HY-170908

Pellotine	5-HT Receptor	Neurological Disease
Pellotine is an alkaloid that can be isolated from Lophophora. Pellotine is the inverse agonist for 5-HT7 receptor with an EC₅₀ of 291 nM. Pellotine exhibits good affinity to *5-HT1DR* and *5-HT6R* with K_i of 117 nM and 170 nM. Pellotine reduces intracellular cAMP levels, thereby reducing neuronal excitability and neurotransmitter release .

HY-174146

5-HT1A agonist 1	5-HT Receptor	Neurological Disease
5-HT1A agonist 1 (Compound Ex.37) is a highly selective 5-HT_1a receptor agonist (EC₅₀=0.18 nM). 5-HT1A agonist 1 mimicks serotonin binding to the receptor, promotes postsynaptic membrane hyperpolarization, inhibits neuronal hyperexcitability, and reduces the release of anxiety-related neurotransmitters. 5-HT1A agonist 1 is promising for research of neuropsychiatric diseases .

HY-W335976

Almotriptan hydrochloride	5-HT Receptor	Neurological Disease
Almotriptan (PNU180638) hydrochloride is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan hydrochloride shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan hydrochloride induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan hydrochloride can be used in research related to migraine.

HY-133858

25N-NBOMe hydrochloride	5-HT Receptor	Neurological Disease
25N-NBOMe hydrochloride, a 2C-N derivative, is a *5-HT2A* and 5-HT2C receptors agonist with K_i 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 .

HY-B0383AS

Almotriptan hydrochloride-d6 PNU180638 hydrochloride-d₆	Isotope-Labeled Compounds 5-HT Receptor	Neurological Disease
Almotriptan-d₆ (PNU180638-d₆) hydrochloride is the deuterium labeled Almotriptan hydrochloride. Almotriptan hydrochloride is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan hydrochloride shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan hydrochloride induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan hydrochloride can be used in research related to migraine.

HY-B0383AS2

Almotriptan-d3 benzoate PNU180638 free base-d₃ benzoate	Isotope-Labeled Compounds 5-HT Receptor	Neurological Disease
Almotriptan-d₃ benzoate (PNU180638 free base-d₃) is deuterated labeled Almotriptan benzoate. Almotriptan benzoate is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan benzoate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan benzoate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan benzoate can be used in research related to migraine.

HY-143797S

Almotriptan-d6 maleate	Isotope-Labeled Compounds 5-HT Receptor	Neurological Disease
Almotriptan-d₆ (PNU180638-d₆) maleate is the deuterium labeled Almotriptan maleate. Almotriptan malate is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine.

Cat. No.	Product Name	Type

HY-D2335

SERTlight

Fluorescent Dyes

SERTlight is a fluorescent agent that can specifically label serotonergic neuronal cell bodies, dendrites, and axonal projections as fluorescent substrates of the serotonin transporter (SERT). SERTlight is orthogonal to various genetically encoded sensors in terms of optics, pharmacology, and operation, enabling multiple imaging. SERTlight allows the use of GRAB_5HT sensors to label distal 5HT axonal projections and simultaneously image the release of endogenous 5HT, providing a new multifunctional molecular tool for studying serotonergic systems .

Cat. No.	Product Name	Target	Research Area

HY-P1422

Spadin 1 Publications Verification	Potassium Channel 5-HT Receptor	Neurological Disease
Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC₅₀ value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research .

HY-P1422A

Spadin TFA 1 Publications Verification	Potassium Channel 5-HT Receptor	Neurological Disease
Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC₅₀ value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research .

HY-P3839

Nocistatin	Opioid Receptor	Neurological Disease
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a G_i/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .

Cat. No.	Product Name	Chemical Structure

HY-12142S

rac-Vofopitant-d3

rac-Vofopitant-d₃ (rac-GR 205171-d₃) is a racemic form of deuterated Vofopitant (HY-12142). Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting .

HY-B0383AS

Almotriptan hydrochloride-d6

Almotriptan-d₆ (PNU180638-d₆) hydrochloride is the deuterium labeled Almotriptan hydrochloride. Almotriptan hydrochloride is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan hydrochloride shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan hydrochloride induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan hydrochloride can be used in research related to migraine.

HY-B0383AS2

Almotriptan-d3 benzoate

Almotriptan-d₃ benzoate (PNU180638 free base-d₃) is deuterated labeled Almotriptan benzoate. Almotriptan benzoate is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan benzoate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan benzoate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan benzoate can be used in research related to migraine.

HY-143797S

Almotriptan-d6 maleate

Almotriptan-d₆ (PNU180638-d₆) maleate is the deuterium labeled Almotriptan maleate. Almotriptan malate is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine.

HY-100656AS

Desmethyl cariprazine-d8

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 serotonin receptors, 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-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.

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