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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
31 Results for "
5-HT receptor subtypes
" in MedChemExpress (MCE) Product Catalog:
Products (31)
31 Results for "5-HT receptor subtypes" in MCE Product Catalog:
2
2 Cited Publications
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
SB-699551 is a selective and brain penetrant 5-HT5A receptor antagonist with a pKi of 8.2 nM. SB-699551 shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 can be used for the research of anxiety, breast cancer, and Alzheimer's disease .
Cat. No.: HY-32329
CAS No.: 57262-94-9
Synonyms: Org-8282
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Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
Synonyms: EGIS-3886
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Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist.
Cat. No.: HY-B1562B
CAS No.: 82857-38-3
Synonyms: (±)-Bopindolol malonate
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Bopindolol ((±)-Bopindolol) malonate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol malonate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol malonate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol malonate is a proagent of Pindolol (HY-B0982). Bopindolol malonate can be used for essential and renovascular hypertension research.
Cat. No.: HY-32329A
CAS No.: 85650-57-3
Synonyms: MO-8282
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Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
Cat. No.: HY-W014208
CAS No.: 503431-81-0
Synonyms: AF-267B
NGX-267 is a selective agonist of the actin M1 receptor, which has high selectivity among the five actin receptor subtypes, especially for the M1 receptor rather than the M3 receptor. NGX-267 also has significant differences in affinity for dopamine D2 and 5-HT2B receptors .
Cat. No.: HY-156807
CAS No.: 210751-39-6
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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 .
Cat. No.: HY-101228
CAS No.: 1407632-07-8
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PSB-12054 is a P2X4 receptor antagonist with IC50 values of 0.19 μM, 2.10 μM and 1.77 μM against human, rat and mouse receptors, respectively, and exhibits selectivity over other human P2X receptor subtypes. PSB-12054 inhibits ATP-induced calcium influx, suppresses shear stress-induced transverse Ca 2+ wave generation, and elevates basal Ca 2+ levels in rat atrial myocytes. PSB-12054 binds to the 5-HT2B receptor. PSB-12054 can be used in research related to neuropathic pain, traumatic brain injury, cerebral ischemia and spinal cord injury .
Cat. No.: HY-124296
CAS No.: 159277-13-1
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2C-TFM hydrochloride is a ,5-dimethoxyphenethylamines compound with a para-trifluoromethyl substitution. 2C-TFM hydrochloride is a potent agonist of the 5-HT receptor subtypes 5-HT2A and 5-HT2C .
Cat. No.: HY-121562
CAS No.: 584555-10-2
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SB 714786 is a potent and selective 5-hydroxytryptamine 1D (5-HT1D) receptor antagonist. It was developed from the previously reported series of dual 5-HT1 selective 5-hydroxytryptamine reuptake inhibitors (5HT1-SSRIs). SB 714786 is the first reported highly potent and selective 5-HT1D receptor antagonist, providing an extremely useful pharmacological tool for further understanding the role of 5-HT1 receptor subtypes. It has no or very low intrinsic activity against all three receptors. SB 714786 has pKi values of 6.5, 6.7, 9.1 and 6.5 for 5-HT1A, 5-HT1B, 5-HT1D and SerT receptors, respectively, showing high selectivity for 5-HT1D receptors. These properties make SB 714786 a potential tool compound for studying the function of 5-HT1D receptors and the treatment of related diseases.
Cat. No.: HY-175532
CAS No.: 3062458-27-6
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M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia
Cat. No.: HY-W505344
CAS No.: 219986-78-4
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Bromo-DragonFLY hydrochloride is an orally active benzodifuran psychoactive substance with hallucinogen-related activity. Bromo-dragonFLY hydrochloride is a 5-HT2A receptor agonist and MAO-A inhibitor that activates the Gαq-PLC-β/IP1/calcium signaling pathway and targets serotonin subtypes associated with hallucinogenic effects. Bromo-dragonFLY hydrochloride produces full substitution for the LSD stimulus in LSD-trained rats in drug discrimination experiments, induces head-twitch responses in mice, and blocks hERG potassium channels. Bromo-dragonFLY hydrochloride can be used in research related to neurological diseases .
Cat. No.: HY-133790
CAS No.: 813425-83-1
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Palonosetron N-oxide is a metabolite of the serotonin (5-HT) receptor subtype 5-HT3 antagonist Palonosetron (HY-A0018).
Cat. No.: HY-117792
CAS No.: 182633-54-1
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LY314228 is an aminoguanidine 5-HT2 antagonist with relative selectivity for 5-HT2A receptors (IC50: 147.9 nM). The Ki values of LY314228 targeting different 5-HT subtypes are 65 nM (5-HT 2A), 1214 nM (5-HT 2B), and 168 nM (5-HT 2C), respectively. LY314228 is an effective inhibitor of 5-HT-induced paw edema in rats with an ED50 of 6.4 mg/kg in ovariectomized female rats. .
Cat. No.: HY-W700240
CAS No.: 177270-91-6
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Triazolomethylindole-3-acetic acid is a metabolite of the serotonin (5-HT) receptor subtype 5-HT1B and 5-HT1D agonist Rizatriptan HY-B0206).
Cat. No.: HY-W740014
CAS No.: 139264-35-0
Synonyms: 183C91; DZT
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N-Desmethyl Zolmitriptan (183C91; DZT) is the active metabolite of the serotonin (5-HT) receptor subtype 5-HT1B and 5-HT1D agonist Zolmitriptan (HY-B0229). N-Desmethyl Zolmitriptan (183C91; DZT) is an agonist of 5-HT1B receptors and induces constriction in isolated human cerebral arteries (EC50=100 nM).
Cat. No.: HY-135774R
CAS No.: 152831-00-0
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1-(Carboxymethyl)cyclohexanecarboxylic acid (Standard) is the analytical standard of 1-(Carboxymethyl)cyclohexanecarboxylic acid. This product is intended for research and analytical applications. 1-(Carboxymethyl)cyclohexanecarboxylic acid (1-Carboxycyclohexaneacetic acid; Gabapentin Impurity E) is a potential impurity in commercial preparations of the antiepileptic agent Gabapentin (HY-A0057). It is also used as a precursor for the synthesis of a serotonin (5-HT) receptor subtype 5-HT2A antagonist.
Cat. No.: HY-100057
CAS No.: 125481-61-0
Synonyms: 6-Hydroxybuspirone; 6'-Hydroxybuspirone; BMS 528215
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BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone (HY-B1115A) and is metabolized by CYP3A4.4. BMY 28674 binds to the serotonin (5-HT) receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe (EC50s are 4 and 1 μM, respectively) and is an antagonist of dopamine D2, D3, and D4 receptors (IC50s are 3.1, 4.9, and 0.85 μM, respectively). BMY 28674 also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner.
Cat. No.: HY-B1562
CAS No.: 62658-63-3
Synonyms: (±)-Bopindolol
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Research Areas:
Bopindolol ((±)-Bopindolol) is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is a proagent of Pindolol (HY-B0982). Bopindolol can be used for essential and renovascular hypertension research.
Cat. No.: HY-B1562C
CAS No.: 79125-22-7
Synonyms: (±)-Bopindolol fumarate
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Bopindolol ((±)-Bopindolol) fumarate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol fumarate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol fumarate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol fumarate is a proagent of Pindolol (HY-B0982). Bopindolol fumarate can be used for essential and renovascular hypertension research.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
