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5-HT Receptor

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Cat. No. Product Name Field of Application Chemical Structure
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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DC78550 TGF-8027
TGF-8027 is a selective 5-HT2A agonist that can cross the blood-brain barrier. TGF-8027 exhibits EC50s of 3.3 nM, 160 nM and 7600 nM against 5-HT2A, 5-HT2C and 5-HT2B and exhibits EC50s against mouse 5-HT2A and mouse 5-HT2C 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-HT2A receptor (such as depression).
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DC78543 Y-36912
Y-36912 is an orally active, highly selective and affinity 5-HT4 receptor agonist (Ki = 1.5 nM). Y-36912 can accelerate gastric emptying and increase bowel frequency and stool weight. Y-36912 can be used for research on gastrointestinal conditions.
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DC78507 MW073
MW073 is a highly selective and orally active 5-HT2BR antagonist (IC50 =70 nM). MW073 exerts its effects by concentration-dependently inhibiting receptor activity and β-arrestin-1 recruitment. MW073 ameliorates synaptic plasticity and behavioral deficits, including aggression, in Alzheimer’s disease (AD) mouse models. MW073 can be used for Alzheimer’s disease (AD) research[1][2].
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DC78504 Elzasonan
Elzasonan (CP-448187) is a 5-hydroxytryptamine1B receptor antagonist. Elzasonan is used in research on depression.
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DC78493 rel-Asenapine hydrochloride
rel-Asenapine (rel-Org 5222) hydrochloride is a relative configuration of Asenapine hydrochloride. Asenapine (Org 5222) hydrochloride, an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine hydrochloride can be used in the research of schizophrenia and bipolar disorder.
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DC78442 SDZ 208-912
SDZ 208-912 is a dual-action 5-HT1A/2 receptor agonist and dopamine D1 receptor antagonist. SDZ 208-912 exhibits partial dopamine agonism and atypical neurosedative effects in rodent models. SDZ 208-912 can be used in research on neurological disorders such as schizophrenia.
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DC78397 SEP-4199
SEP-4199 is a nonracemic 85:15 ratio of Aramisulpride and Esamisulpride. SEP-4199 exhibits significant differences in relative potency at two different receptors (5-HT7R and D2R) compared to the racemate. SEP-4199 exhibits antidepressant effects.
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DC78322 GSK-958108
GSK-958108 is a highly selective 5-HT1A receptor antagonist. GSK-958108 is commonly used in the study of neurological conditions.
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DC78317 MCI-225 hydrate hydrochloride
MCI-225 (DDP-225) hydrate hydrochloride is a selective and orally active noradrenaline (NA) reuptake inhibitor with 5-HT3 receptor antagonism. MCI-225 hydrate hydrochloride has antidepressant-like and anxiolytic-like properties. MCI-225 hydrate hydrochloride can be used for the study of anxiety disorder.
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