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Results for "

5-HT responses

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (39) Adrenergic Receptor (5) Androgen Receptor (1) Arrestin (1) COX (2) Dopamine Receptor (6) Drug Derivative (4) Drug Isomer (2) EGFR (1) G protein-coupled Bile Acid Receptor 1 (1) Histamine Receptor (2) iGluR (1) Isotope-Labeled Compounds (4) mAChR (2) Neurokinin Receptor (3) PKA (1) Reference Standards (5) Serotonin Transporter (6) Sigma Receptor (2) Sodium Channel (1) Transthyretin (TTR) (2)
By Research Areas:	Cancer (2) Cardiovascular Disease (4) Endocrinology (2) Inflammation/Immunology (2) Metabolic Disease (3) Neurological Disease (39)

By Targets:

5-HT Receptor (39)

Adrenergic Receptor (5)

Androgen Receptor (1)

Arrestin (1)

COX (2)

Dopamine Receptor (6)

Drug Derivative (4)

Drug Isomer (2)

EGFR (1)

G protein-coupled Bile Acid Receptor 1 (1)

Histamine Receptor (2)

iGluR (1)

Isotope-Labeled Compounds (4)

mAChR (2)

Neurokinin Receptor (3)

PKA (1)

Reference Standards (5)

Serotonin Transporter (6)

Sigma Receptor (2)

Sodium Channel (1)

Transthyretin (TTR) (2)

By Research Areas:

Cancer (2)

Cardiovascular Disease (4)

Endocrinology (2)

Inflammation/Immunology (2)

Metabolic Disease (3)

Neurological Disease (39)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: 5-HT Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N1957

Gamma-Mangostin 2 Publications Verification γ-Mangostin	5-HT Receptor COX Transthyretin (TTR)	Metabolic Disease Inflammation/Immunology Cancer
Gamma-Mangostin is a novel competitive *5-hydroxytryptamine 2A (5-HT2A) receptor* antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3 ^H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .

HY-15574

Piboserod 4 Publications Verification SB-207266	5-HT Receptor	Cardiovascular Disease
Piboserod is an orally available selective antagonist of the 5-HT4 receptor, with a K_i value of approximately 0.1 nM for human 5-HT4 receptors. Piboserod can competitively bind to the 5-HT4 receptor and block the activation of the 5-HT4 receptor. Piboserod can inhibit the enhancing effect of 5-HT on the nerve-mediated contraction response of the human bladder detrusor muscle. Piboserod is mainly used in the research of urinary system diseases (such as overactive bladder) and cardiovascular diseases (such as chronic heart failure) .

HY-169841

IHCH-7086	5-HT Receptor Arrestin	Neurological Disease
IHCH-7086 is a blood-brain barrier-permeable, partial β-arrestin-biased agonist of *5-HT_2AR* with a K_i of 12.59 nM. IHCH-7086 blocks D-lysergic acid diethylamide-induced head-twitch response in mice and alleviates depression-like behaviors in mice subjected to acute restraint stress or injected with Corticosterone (HY-B1618). IHCH-7086 is applicable to research related to depression .

HY-110023

Zimelidine dihydrochloride	Serotonin Transporter	Neurological Disease
Zimelidine dihydrochloride is an orally active selective serotonin reuptake inhibitor. Zimelidine dihydrochloride competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine dihydrochloride time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine dihydrochloride strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine dihydrochloride exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine dihydrochloride is used for the study of depressive disorders and analgesic tolerance .

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-N0775

Isocorynoxeine 1 Publications Verification 7-Isocorynoxeine	5-HT Receptor	Neurological Disease
Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of *5-HT_2A* receptor-mediated current response with an IC₅₀ of 72.4 μM.

HY-138218

ALD-52 1-Acetyl-LSD	Drug Derivative 5-HT Receptor	Neurological Disease
ALD-52 (1-Acetyl-LSD) is a prodrug for LSD. ALD-52 shows an affinity to 5-HT_1A, 5-HT_2A and 5-HT_2C with a sub>D values of 1054, 174 and 10.2 nM, respectively. ALD-52 is converted to LSD and induces a head-twitch response (HTR) in vivo. ALD-52 can be used for hallucinogen research .

HY-106584

Mosapramine Clospipramine	Drug Derivative Dopamine Receptor 5-HT Receptor	Neurological Disease
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 .

HY-13200

BRL-15572 dihydrochloride	5-HT Receptor	Neurological Disease
BRL-15572 dihydrochloride is a selective antagonist of *h5-HT1D, displays high affinity for h5-HT1D* receptors. BRL-15572 dihydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses .

HY-103101

LP44 hydrochloride	5-HT Receptor	Others
LP44 (hydrochloride) is a selective *5-HT7* agonist with Ki of 0.22 nM. LP44 (hydrochloride) induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 (hydrochloride) not causes considerable hypothermic response by intraperitoneal administration .

HY-100923

H-9 Dihydrochloride	PKA 5-HT Receptor EGFR	Neurological Disease
H-9 Dihydrochloride is a PKA (protein kinase) inhibitor. H-9 Dihydrochloride (10 μM) significantly reduces the excitatory response to *5-HT*. H-9 Dihydrochloride also has a direct effect on pharyngeal activity. H-9 Dihydrochloride inhibits signal-transduction and cell growth in EGF (epidermal growth factor)-dependent epithelial cell lines .

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-178760

TGF-8027	5-HT Receptor	Neurological Disease
TGF-8027 is a selective *5-HT_2A* agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC₅₀s of 3.3 nM, 160 nM and 7600 nM against human *5-HT_2A, 5-HT_2C* and *5-HT_2B* and exhibits EC₅₀s against mouse 5-HT_2A and mouse 5-HT_2C of 14 and 210 nM. TGF-8027 can induce a head-shaking response in mice. TGF-8027 can be used to study diseases that target the 5-HT_2A receptor (such as depression) .

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-135439

SB-203186	5-HT Receptor	Neurological Disease
SB-203186 is a highly selective 5-HT₄ receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pK_B value being 8.3 in the isolated right atrium model of piglets. SB-203186 can dose-dependently shift the 5-HT-induced tachycardia curve to the right, and does not inhibit the maximum response. SB-203186 is an efficient 5-HT₄ antagonist in pig and human atria, but has no significant inhibitory effect in rat atria. SB-203186 can be used for the study of diseases such as arrhythmias and abnormal myocardial contraction .

HY-162423

CYB210010	5-HT Receptor Androgen Receptor	Neurological Disease
CYB210010 is an orally bioavailable, long-acting serotonin *5-HT2* receptor agonist that selectively targets 5-HT2A and 5-HT2C receptors (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 .

HY-118835

Zimelidine	Serotonin Transporter	Neurological Disease
Zimelidine is an orally active selective serotonin reuptake inhibitor. Zimelidine competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine is used for the study of depressive disorders and analgesic tolerance .

HY-165624A

(S)-LY-41	Drug Isomer Drug Derivative 5-HT Receptor	Neurological Disease
(S)-LY-41, R-enantiomer of LY-41 (HY-165624), is 2-Sminotetralin (HY-W022362) derivative and 8-OH-DPAT (HY-112061) analogue. (S)-LY-41 is a potent and selective 5-HT1A receptor agonist. (S)-LY-41 can reduce the accumulation of 5-hydroxytryptophan (the precursor for 5-HT synthesis) in the rat brain induced by decarboxylase inhibitors (NSD 1015). (S)-LY-41 can lower the body temperature of rats and inhibit the escape response from the cage. (S)-LY-41 can induce the 5-HT behavioral syndrome. (S)-LY-41can be used for the research of neurological disease, such as depression and anxiety .

HY-165624B

(R)-LY-41	Drug Isomer Drug Derivative 5-HT Receptor	Neurological Disease
(R)-LY-41, R-enantiomer of LY-41 (HY-165624), is 2-Sminotetralin (HY-W022362) derivative and 8-OH-DPAT (HY-112061) analogue. (R)-LY-41 is a potent and selective 5-HT1A receptor agonist. (R)-LY-41 can reduce the accumulation of 5-hydroxytryptophan (the precursor for 5-HT synthesis) in the rat brain induced by decarboxylase inhibitors (NSD 1015). (R)-LY-41 can lower the body temperature of rats and inhibit the escape response from the cage. (R)-LY-41 can induce the 5-HT behavioral syndrome but is weaker than (S)-LY-41 (HY-165624A). (R)-LY-41 can be used for the research of neurological disease, such as depression and anxiety .

HY-106605

Flumezapine LY 120363	Dopamine Receptor 5-HT Receptor	Neurological Disease
Flumezapine (LY 120363) is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine can be used in antipsychotic research .

HY-100552

VUF10166	5-HT Receptor	Neurological Disease
VUF10166 is a potent and high-affinity 5-HT₃ receptor antagonist, with K_i values of 0.04 nM (5-HT₃A) and 22 nM (5-HT₃AB). VUF10166 inhibits 5-HT-induced responses at 5-HT₃A and 5-HT₃AB receptors at nanomolar concentrations. At 5-HT₃ receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC₅₀ of 5.2 μM .

HY-113866

E-55888	5-HT Receptor	Neurological Disease
E-55888 is a selective and potent agonist of 5-HT₇ receptor and 5-HT_1A receptor with K_i values of 2.5 nM and 700 nM, respectively, which has analgesic and antinociceptive effects. E-55888 reduces the nociceptive response of Capsaicin (HY-10448) sensitized mice .

HY-A0139

Thiothixene NSC 108165; Navan; Navane	Sigma Receptor mAChR Histamine Receptor Dopamine Receptor Adrenergic Receptor	Others
Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.

HY-111291

ICI 169369 free base	5-HT Receptor	Neurological Disease Endocrinology
ICI 169369 (free base) is an orally active, selective and non-competitive antagonist against 5HT receptor. ICI 169369 (free base) blunts the vasopressin (AVP), but not the ACTH, prolactin or growth hormone reponses to insulin-induced hypoglycaemia. ICI 169369 (free base) blocks centrally mediated 5-HT responses and lowers portal pressure in portal hypertensive rats .

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-123514

SNAP8719 free base	Adrenergic Receptor Dopamine Receptor 5-HT Receptor	Others
SNAP8719 free base is a selective α_1D-adrenoceptor antagonist (pK_i = 8.89). SNAP8719 free base shows affinity for the dopamine D₂-, *5-HT_1A-, and the human clonal α_2a-adrenoceptor, with pK_i* values of 5.98, 6.47, and <5.0, respectively. SNAP8719 free base causes a concentration-dependent increase in the twitch response .

HY-N1957R

Gamma-Mangostin (Standard) γ-Mangostin (Standard)	Reference Standards 5-HT Receptor COX Transthyretin (TTR)	Metabolic Disease Inflammation/Immunology Cancer
Gamma-Mangostin (Standard) is the analytical standard of Gamma-Mangostin. This product is intended for research and analytical applications. Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .

HY-P1441A

Mambalgin 1 TFA	Sodium Channel	Neurological Disease
Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC₅₀ values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.

HY-110023R

Zimelidine dihydrochloride (Standard)	Reference Standards Serotonin Transporter	Neurological Disease
Zimelidine dihydrochloride (Standard) is the analytical standard of Zimelidine dihydrochloride (HY-110023). This product is intended for research and analytical applications. Zimelidine dihydrochloride is an orally active selective serotonin reuptake inhibitor. Zimelidine dihydrochloride competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine dihydrochloride time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine dihydrochloride strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine dihydrochloride exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine dihydrochloride is used for the study of depressive disorders and analgesic tolerance .

HY-118835S

Zimeldine-d6	Isotope-Labeled Compounds Serotonin Transporter	Neurological Disease
Zimeldine-d₆ is the deuterium labeled Zimeldine (HY-118835) . Zimelidine is an orally active selective serotonin reuptake inhibitor. Zimelidine competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine is used for the study of depressive disorders and analgesic tolerance .

HY-115375

R 50595 hydrochloride	5-HT Receptor	Neurological Disease
50595 hydrochloride is a selective noncompetitive cisapride antagonist that interferes with the activity of cisapride and BRL 24924. R 50595 hydrochloride has no effect on the response to electrical stimulation at concentrations up to 3 X 10(-7) M. R 50595 hydrochloride antagonizes the effects of cisapride and BRL 24924 in a noncompetitive manner. R 50595 hydrochloride completely abolishes the effects of 5-HT at a concentration of 3 X 10(-7) M and also antagonizes the effects of 5-HT in a noncompetitive manner .

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-160921

Capeserod SL65.0155 free base	5-HT Receptor	Neurological Disease
Capeserod (SL65.0155 free base) is an agonist for serotonin receptor (5-HT receptor), with a K_i of 0.6 nM for 5-HT₄ receptor. Capeserod enhances expression of phopshorilated cAMP-response element binding protein (p-CREB), vascular endothelium growth factor (VEGF), brain-derived neurotrophic factor (BDNF) and B cell lymphoma-2 (Bcl-2) proteins in hippocampus, and exhibits antidepressant-like efficacy in Wistar rats models .

HY-15574R

Piboserod (Standard) SB-207266 (Standard)	5-HT Receptor Reference Standards	Cardiovascular Disease
Piboserod (Standard) is the analytical standard of Piboserod. This product is intended for research and analytical applications. Piboserod is an orally available selective antagonist of the 5-HT4 receptor, with a Ki value of approximately 0.1 nM for human 5-HT4 receptors. Piboserod can competitively bind to the 5-HT4 receptor and block the activation of the 5-HT4 receptor. Piboserod can inhibit the enhancing effect of 5-HT on the nerve-mediated contraction response of the human bladder detrusor muscle. Piboserod is mainly used in the research of urinary system diseases (such as overactive bladder) and cardiovascular diseases (such as chronic heart failure) .

HY-117063

LEK 8841 methanesulfonate	5-HT Receptor	Endocrinology
LEK 8841 methanesulfonate is a gastrointestinal calming agent with strong selective 5-HT2 receptor antagonist activity. The antipsychotic potential of LEK 8841 has made it the focus of research into alternative medicines. LEK 8841 behaves as a pure competitive antagonist in response to 5-HT and norepinephrine, with pA2 values of 7.93 and 6.45, respectively. The selectivity of LEK 8841 is better than that of the comparative drug ketanserin, making it an important reference value in corresponding receptor research. Studies related to structural modifications have shown that LEK 8841 exhibits high affinity for 5-HT2 receptors and low alpha-adrenergic receptor activity .

HY-106605S

Flumezapine-d8 hydrochloride LY 120363-d8 hydrochloride	Isotope-Labeled Compounds Dopamine Receptor 5-HT Receptor	Neurological Disease
Flumezapine-d₈ (LY 120363-d₈) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.

HY-118775

LEK 8804	5-HT Receptor	Others
LEK 8804 is a compound with 5-HT1A receptor agonist and 5-HT2 receptor antagonist properties, and has the activity of modulating related receptor-mediated behavioral responses. LEK 8804 can induce spontaneous tail-flick response in rats in a dose-dependent manner, showing complete 5-HT1A agonist activity, and can inhibit 5-HTP-induced head twitch response in mice, probably through antagonism of 5-HT2 receptors rather than agonism of 5-HT1A receptors.

HY-13200B

BRL-15572	5-HT Receptor	Neurological Disease
BRL-15572 is a selective antagonist of *h5-HT1D, displays high affinity for h5-HT1D* receptors. BRL-15572 could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses .

HY-13200A

BRL-15572 hydrochloride	5-HT Receptor	Neurological Disease
BRL-15572 hydrochloride is a selective antagonist of *h5-HT1D, displays high affinity for h5-HT1D* receptors. BRL-15572 hydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses .

HY-146232

F 13714 F 14679	5-HT Receptor	Others
F 13714 (F 14679) is a prototypical *5-HT_1A* agonist with a pK_i of 10.23. F 13714 induces large Ca ²⁺ responses .

HY-169446

ALEPH hydrochloride	5-HT Receptor	Neurological Disease
ALEPH (hydrochloride) is the *h5-HT_2A* and *h5-HT_2B* partial agonist with the EC₅₀ values of 10.3 nM and 19.2 nM, respectively. ALEPH (hydrochloride) causes head twitch response in mice (ED₅₀: 0.80 mg/kg) .

HY-122303

4-hydroxy DiPT hydrochloride 4-OH-DiPT hydrochloride	5-HT Receptor	Neurological Disease
4-hydroxy DiPT hydrochloride is an *5-HT_2A* agonist that induces the head-twitch response (HTR) in mice, indicating psychoactivity . 4-hydroxy DiPT hydrochloride significantly reduced freezing responses to conditioned cues in a dose-dependent manner with a greater potency in female mice than male mice .

HY-N0775R

Isocorynoxeine (Standard) 7-Isocorynoxeine (Standard)	Reference Standards 5-HT Receptor	Neurological Disease
Isocorynoxeine (Standard) is the analytical standard of Isocorynoxeine. This product is intended for research and analytical applications. Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.

HY-121704

SR 57227A free base	iGluR	Neurological Disease
SR 57227A Free base is a highly selective compound for both peripheral and central 5-HT3 receptors and acts as an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells, demonstrating antidepressant-like effects in rats while reducing isolation-induced aggressive behavior.

HY-W748758

(Z)-Thiothixene-d8 NSC 108165-d₈; Navan-d₈; Navane-d₈	Isotope-Labeled Compounds Dopamine Receptor Histamine Receptor mAChR Adrenergic Receptor Sigma Receptor	Others
(Z)-Thiothixene-d₈ (NSC 108165-d₈; Navan-d₈; Navane-d₈) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.

HY-182472

AL-38022A	5-HT Receptor	Neurological Disease
AL-38022A is a potent and selective 5-HT₂ receptor agonist (K_i ≤2.2 nM), but a significantly lower (>100-fold less) affinity for other 5-HT receptors. AL-38022A potently stimulates functional responses via 5-HT₂ receptor subtypes including [Ca ²⁺]_i mobilization and tissue contractions with apparently similar potencies and intrinsic activities. AL-38022A fully generalizes to the (±)-1-(2,5-dimethoxy 4-methylphenyl)-2-aminopropane hydrochloride (DOM) stimulus in drug discrimination paradigms. AL-38022A can be used for the glaucoma research .

HY-181878

Z8779877149 Z7149	Serotonin Transporter Adrenergic Receptor 5-HT Receptor	Neurological Disease
Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (K_i=198 nM), α2A adrenergic receptor (K_i=180 nM; EC₅₀=440 nM) and *5-HT_2A* receptor (EC₅₀=172 nM, E_max=76%). Z8779877149 inhibits *5-HT* reuptake and activates G_i and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders .

HY-182584

S 15931	5-HT Receptor	Neurological Disease
S 15931 is a *5-HT_1A* receptor inhibitor. S 15931 inhibits the late-phase hindpaw licking response induced by formalin and the abdominal writhing response induced by acetic acid in Mus musculus. S 15931 abolishes the spontaneous tail-flick response induced by 8-OH-DPAT in Rattus norvegicus and potentiates the analgesic effect of morphine. S 15931 is applicable for pain-related research .

HY-180185

5-HT2A&5-HT2C agonist-2	5-HT Receptor	Neurological Disease Metabolic Disease
5-HT2A&5-HT2C agonist-2 (Compound 3ci) is a highly selective dual *5-HT2A/5-HT2C* agonist that can cross the blood-brain barrier and has an EC₅₀ < 1 μM. 5-HT2A&5-HT2C agonist-2 has high selectivity for 5-HT2B related to the risk of heart valve disease. 5-HT2A&5-HT2C agonist-2 can induce head convulsive responses, but has a relatively low hallucinogenic potential. 5-HT2A&5-HT2C agonist-2 can be used in the research of diseases such as depression and obesity .

HY-103101R

LP44 hydrochloride (Standard)	Reference Standards 5-HT Receptor	Others
LP44 hydrochloride (Standard) is the analytical standard of LP44 hydrochloride (HY-103101). This product is intended for research and analytical applications. LP44 hydrochloride is a selective 5-HT7 agonist with K_i of 0.22 nM. LP44 hydrochloride induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 hydrochloride not causes considerable hypothermic response by intraperitoneal administration .

Cat. No.	Product Name	Target	Research Area

HY-P1441A

Mambalgin 1 TFA	Sodium Channel	Neurological Disease
Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC₅₀ values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N1957

Gamma-Mangostin 2 Publications Verification γ-Mangostin	Xanthones Classification of Application Fields Guttiferae Phenols Polyphenols Garcinia mangostana Linn. Metabolic Disease Plants Disease Research Fields	5-HT Receptor COX Transthyretin (TTR)
Gamma-Mangostin is a novel competitive *5-hydroxytryptamine 2A (5-HT2A) receptor* antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3 ^H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .

HY-N0775

Isocorynoxeine 1 Publications Verification 7-Isocorynoxeine	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Alkaloids Rubiaceae Plants Indole Alkaloids Source Classification	5-HT Receptor
Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of *5-HT_2A* receptor-mediated current response with an IC₅₀ of 72.4 μM.

HY-N1957R

Gamma-Mangostin (Standard) γ-Mangostin (Standard)	Structural Classification Xanthones Guttiferae Phenols Polyphenols Garcinia mangostana Linn. Plants	Reference Standards 5-HT Receptor COX Transthyretin (TTR)
Gamma-Mangostin (Standard) is the analytical standard of Gamma-Mangostin. This product is intended for research and analytical applications. Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer . Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .

HY-N0775R

Isocorynoxeine (Standard) 7-Isocorynoxeine (Standard)	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Alkaloids Structural Classification Rubiaceae Plants Indole Alkaloids Source Classification	Reference Standards 5-HT Receptor
Isocorynoxeine (Standard) is the analytical standard of Isocorynoxeine. This product is intended for research and analytical applications. Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.

Cat. No.	Product Name	Chemical Structure

HY-118835S

Zimeldine-d6

Zimeldine-d₆ is the deuterium labeled Zimeldine (HY-118835) . Zimelidine is an orally active selective serotonin reuptake inhibitor. Zimelidine competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine is used for the study of depressive disorders and analgesic tolerance .

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-106605S

Flumezapine-d8 hydrochloride

Flumezapine-d₈ (LY 120363-d₈) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.

HY-W748758

(Z)-Thiothixene-d8

(Z)-Thiothixene-d₈ (NSC 108165-d₈; Navan-d₈; Navane-d₈) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.

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