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Home > Inhibitors & Agonists > GPCR > 5-HT Receptor

5-HT Receptor

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Cat. No. Product Name Field of Application Chemical Structure
DC79787 5-Hydroxy-6-methoxy (S)-duloxetine maleate
5-Hydroxy-6-methoxy (S)-duloxetine maleate is an orally active and brain-penetrant serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with antidepressant and analgesic activities. 5-Hydroxy-6-methoxy (S)-duloxetine maleate is promising for research of psychiatric and neurological disorders such as depression, diabetic neuropathic pain, generalized anxiety disorder, and fibromyalgia.
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DC79757 TKS 159
TKS 159 is a 5-HT4 receptor agonist. TKS 159 can promote gastrointestinal motility. TKS 159 can be used for research on gastrointestinal conditions.
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DC79678 SB 258741
SB 258741 is an efficient and highly selective 5-HT7 receptor (pKi = 8.
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DC79659 BVT-74316
BVT-74316 is a 5-HT6 receptor antagonist. BVT-74316 can reduce food intake and bodyweight gain in rodent models. BVT-74316 can be used for the research of metabolic disease, such as obesity.
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DC79621 Batoprazine
Batoprazine (8-(1-piperazinyl)-2H-1-benzopyran-2-one)) is a 5-HT1A,1B receptor agonist. Batoprazine can replace the behavioral stimulus of eltoprazine in the two-lever operant discrimination test between eltoprazine and deionized water in rats (ED50: 0.20 mg/kg).
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DC79614 GSK-163090 dihydrochloride
GSK-163090 (dihydrochloride) is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4, 8.5 and 9.7, respectively. GSK-163090 (dihydrochloride) inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK-163090 (dihydrochloride) has antidepressant and anxiolytic activities.
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DC79410 BMS-505130 fumarate
BMS-505130 (fumarate) is a potent, selective and orally active serotonin transport inhibitor with a Ki for binding to the serotonin transporter of 0.18 nM (Ki for norepinephrine and dopamine transporters of 4.6 and 2.1 μM, respectively). BMS-505130 (fumarate) can be used for the research of neurological disease, such as depression.
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DC79407 KW-5092 (fumarete)
KW-5092 (fumarete) is a gastrokinetic agent. KW-5092 (fumarete) can increase intraluminal 5-HT release via the stimulation of cholinergic neurons .
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DC79346 RS-56812
RS-56812 is a partial agonist of the 5-HT3 receptor. RS-56812 significantly enhances the propulsive peristalsis of the colon. RS-56812 indirectly enhances cholinergic neurotransmission and improves the working memory performance of non-human primates. RS-56812 is used in research on diarrhea/colon peristalsis and cognitive disorders (such as Alzheimer's disease).
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DC79321 GR 55562
GR 55562 is a selective 5-HT1B receptor antagonist. GR 55562 can be used for the research of nerve disease.
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DC79283 SB-247853
SB-247853 is a highly specific 5-HT2c receptor antagonist. SB-247853 induces orthostatic intolerance during head-up tilting. SB-247853 can be used in the research of cardiovascular diseases.
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DC79166 Luvesilocin
Luvesilocin (Example 6) is a tryptamine prodrug. Luvesilocin can convert into an active form, acting as a 5HT2A agonist in vivo upon administration. Luvesilocin can be studied in research for mental diorders.
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DC79125 SB-203186
SB-203186 is a highly selective 5-HT4 receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pKB 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.
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DC79086 LY334370 fumarate
LY334370 fumarate is the fumarate of LY334370). LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM.
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DC79085 IHCH-7179
IHCH-7179 is a 5-HT receptor modulator. IHCH-7179 can antagonize 5-HT2A receptor and activate 5-HT1A receptor. IHCH-7179 can be used for the research of neurological disease.
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DC78856 R 116712
R 116712 is a highly selective and affinity 5-HT4 receptor ligand. R 116712 can prepare isotopic markers.
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DC78838 2-(2-Methoxyphenoxy)ethylamine hydrochloride
2-(2-Methoxyphenoxy)ethylamine hydrochloride (Compound 2b) is a mixed agonist/antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride is a5-HT1A receptor partial agonist and a α1-adrenergic receptor antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride can be used for neurological diseases research, such as anxiety, depression and psychosis.
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DC78824 5-Benzyloxytryptamine
5-Benzyloxytryptamine (5-BT) is a selective partial agonist for 5-hydroxytryptamine 1D/1B (5-HT1D/1B) receptors with an IC50 value of 40 nM for bovine caudate 5-HT1D and reduced affinity for other receptors (5-HT2 IC50>470 nM). 5-Benzyloxytryptamine inhibits adenylate cyclase to decrease neurotransmitter release and downregulate cAMP signaling. 5-Benzyloxytryptamine is promising for research of neurotransmitter imbalance-related disorders like migraine.
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DC78823 L694247 TFA
L694247 (TFA) is a selective 5-HT1D agonist with pIC50 values of 10.03, 8.64, 6.42, and 5.66 for 5-HT1D, 5-HT1A, 5-HT1C, and 5-HT1E receptors, respectively.
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DC78760 LY-228729
LY-228729 is a selective 5-HT1A receptor agonist. LY-228729 can reduce the rearing frequency of rats and decrease their activity in the central area in the open field test. LY-228729 can reduce the immobility time of rats and increase their swimming time in the forced swim test. LY-228729 can be used in the research of neurological diseases.
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DC78758 U 93385
U93385 is a 5-HT₁A receptor agonist. U93385 exhibits no significant α₂ adrenergic, D₂ dopamine, or other receptor activities. U93385 has a heart rate regulating effect, stimulating the vagus nerve to induce bradycardia. U93385 can be used to study the 5-HT₁A receptor-mediated vagal nerve tolerance mechanism.
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DC78742 BP 554
BP 554 is a selective 5-HT1A receptor agonist and Piperazine derivative. BP 554 leads to hypothermia.
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DC78717 EMD 86006
EMD 86006 is a candidate for selective serotonin inhibitors. EMD 86006 has the potential for research on depressive disorders.
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DC78706 RS 2232
RS 2232 is an orally active, competitive 5-HT deamination inhibitor with a Ki of 0.054 μM. RS-2232 exhibits reversible and specific inhibition of type A monoamine oxidase. RS 2232 can be used in brain research.
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DC78685 BMS-181101 hydrochloride
BMS-181101 (hydrochloride) is an orally active antidepressant. BMS-181101 (hydrochloride) can interact with a variety of central presynaptic and postsynaptic 5-HT receptors. BMS-181101 (hydrochloride) can be used in the research of diseases such as depression.
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DC78662 R 1485 dihydrochloride
R 1485 is a 5-HT6 receptor antagonist.
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DC78654 MARY1
MARY1 is a selective 5-HT2BR antagonist with an IC50 of 380 nM and a Ki of 764 nM (human 5-HT2BR). MARY1 induces renal mitochondrial biogenesis (MB) and enhances renal mitochondrial function by increasing mitochondrial respiratory capacity, mitochondrial protein levels, and mitochondrial number in renal proximal tubular cells (RPTCs). MARY1 induces MB through 5-HT2BR and dual PI3K/AKT and RAS/MEK/ERK cell signaling pathways in RPTCs. MARY1 can be used to study renal diseases associated with metabolic and mitochondrial dysfunction.
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DC78596 ST171
ST171 is a bitopic 5-HT1AR agonist with an Ki of 0.41  nM. ST171 selectively activates Gi/o signaling pathway and inhibits 5-HT1AR-mediated cAMP accumulation without Gs activation and marginal β-arrestin recruitment. T171 reduces hypersensitivity in chronic neuropathic and inflammatory pain mice model. ST171 can be used for pain research.
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DC78576 5-HT2AR ligand 1
5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT2AR ligand with nanomolar affinity for 5-HT2AR (Ki: 32 nM). 5-HT2AR ligand 1 is capable of inducing β-arrestin 2 recruitment. 5-HT2AR ligand 1 can be used in the research of neurological diseases.
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DC78554 F-14258
F-14258 is a 5-HT1B/1D receptor agonist. F-14258 can achieve receptor specific analgesia through local administration. F-14258 can be used for research on ear pain.
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