serotonin 3 receptor

Facinicline hydrochloride (RG3487) 是一种口服有效的烟碱α7 receptor 部分激动剂，对人 nAChR 的 Ki 值为 6 nM。它可改善啮齿类动物的认知和感觉运动门控。它与5-HT3受体结合的 Ki 为 1.2 nM。

Granisetron hydrochloride (Granisetron HCl) 是一种5-HT3受体拮抗剂，可作为化疗后止吐剂。

Tropisetron hydrochloride (Tropisetron HCl) 是5-HT3受体拮抗剂和α7-烟碱受体激动剂，具有抗恶心和止吐活性，对5-HT3受体的 IC50为70.1 nM。

LY334370 是一种选择性5-HT1F 受体激动剂，Ki 值为 1.6 nM。

RU 24969 (5-methoxy-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole) 是 5-HT1A 和 5-HT1B 受体的选择性激动剂，Ki 值分别为 0.38 和 2.5 nM。它可减少液体消耗并增加向前运动。

(2-methylpropyl)({[3-(trifluoromethyl)phenyl]methyl})amine 是一种选择性血清素受体激动剂，特异性靶向5-HT2A 和5-HT2C 受体，已被用于研究血清素在各种生理和病理条件下的作用。

3-(2-aminopropyl)phenol hydrochloride 是一种用作分子结构单元的苯乙胺类化合物。它是一种精神活性药物，是5-HT1A、5-HT1B 和5-HT2C 等几种血清素受体的部分激动剂，也是5-HT2A 受体的拮抗剂。

2-(5,7-dichloro-1H-indol-3-yl)ethan-1-amine 是一种吲哚胺类化合物，在结构上与血清素相似。它是5-HT2A 受体的选择性激动剂，在神经科学领域具有潜在的应用。

AM9405是一种新型的外周活性大麻素1型 (CB1)和5-羟色胺3型受体激动剂。 AM9405抑制回肠和结肠的抽搐收缩，IC50分别为45.71 和 0.076 nM。AM9405 在生理条件下显着减缓小鼠肠道蠕动.

Ondansetron hydrochloride dihydrate (GR 38032) 是5- HT3受体拮抗剂，可治疗化疗后的恶心和呕吐，有抗焦虑和抗精神病作用。

HDAC6-IN-49（Compound 3）作为HDAC的抑制剂，针对HDAC6与HDAC1的IC50值分别为0.012 μM和0.735 μM。此化合物还能够抑制MAO-B、胆碱酯酶 (ChE)、组胺受体 (H3R)以及血清素6受体 (5-HT6R)。在生物学应用方面，HDAC6-IN-49对SH-SY5Y细胞展示出神经保护效果，并在果蝇的帕金森病模型与C. elegans的阿尔茨海默病模型中改善了认知功能与运动能力。

25CN-NBMD作为一种高度选择性的血清素5-HT2A受体(5-HT2AR)激动剂，被开发用于探索5-HT2AR的表达及功能。在25CN-NBMD的2'与3'位点进行了结构修饰，研究发现这些改变对5-HT2AR活性至关重要。此化合物在诱导与5-HT2AR激活相关的特征反应方面显示出有效性。

Triazolomethylindole-3-acetic acid 是 Rizatriptan 的代谢物，该化合物作用于血清素 (5-HT) 受体亚型 5-HT1B 和 5-HT1D 作为激动剂。

Granisetron, a serotonin receptor (5HT-3 selective) antagonist, is used as an antinauseant and antiemetic for cancer chemotherapy.

Indisetron Dihydrochloride is a 5-HT(3) and 5-HT(4) receptor antagonist. Indisetron reduces 2-methyl-5-serotonin (HT)-induced bradycardia.

JNJ-28583867 is an inhibitor of histamine H(3) receptor antagonist and serotonin reuptake.

Donecopride is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT4E(Ki= 8.5 nM) and an inhibitor of acetylcholinesterase (AChE; IC50= 16 nM).1It is selective for AChE over butyrylcholinesterase (BChE; IC50= 3,530 nM) but does bind to 5-HT2Band sigma-2 (σ2) receptors (Ki= 1.6 nM for both) in a panel of 42 neurotransmitter receptors and transporters. Donecopride induces release of soluble amyloid precursor protein-α (sAPP-α) in COS-7 cells transiently expressing 5-HT4with an EC50value of 11.3 nM. Oral administration of donecopride (1 mg/kg) reduces brain soluble and insoluble amyloid-β (1-42) levels and increases the time spent exploring the novel object in the novel object recognition (NOR) test in the 5XFAD transgenic mouse model of Alzheimer's disease. Donecopride (3 mg/kg, p.o.) prevents a reduction in spontaneous alternation behavior induced by intracerebroventricular administration of soluble Aβ42 (sAβ42) in the Y-maze in mice.2 1.Lecoutey, C., Hedou, D., Freret, T., et al.Design of donecopride, a dual serotonin subtype 4 receptor agonist/acetylcholinesterase inhibitor with potential interest for Alzheimer's disease treatmentProc. Natl. Acad. Sci. USA111(36)E3825-E3830(2014) 2.Rochais, C., Lecoutey, C., Hamidouche, K., et al.Donecopride, a Swiss army knife with potential against Alzheimer's diseaseBr. J. Pharmacol.177(9)1988-2005(2020)

Palonosetron N-oxide is a metabolite of the serotonin (5-HT) receptor subtype 5-HT3antagonist palonosetron .1It is also a potential impurity in palonosetron preparations.2Palonosetron N-oxide is a degradation product formed by exposure to oxidative stress. 1.Stoltz, R.A., Cyong, J.-C., Shah, A., et al.Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjectsJ. Clin. Pharmacol.44(5)520-531(2004) 2.Vishnu Murthy, M., Srinivas, K., Kumar, R., et al.Development and validation of a stability-indicating LC method for determining palonosetron hydrochloride, its related compounds and degradation products using naphthalethyl stationary phaseJ. Pharm. Biomed. Anal.56(2)429-435(2011)

Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A 1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of non-specific binding [1]. Eltoprazine evoked membrane changes that were similar to but much weaker than those induced by 5HT. Both the 5HT- and eltoprazine-evoked membrane hyperpolarizations were largely suppressed in the presence of spiperone [2].in vivo: eltoprazine is extremely effective in suppressing dyskinesia in experimental models, although this effect was accompanied by a partial worsening of the therapeutic effect of l-dopa. Interestingly, eltoprazine was found to (synergistically) potentiate the antidyskinetic effect of amantadine. The current data indicated that eltoprazine is highly effective in counteracting dyskinesia in preclinical models [3]. Rats were chronically treated with mianserin (10 mg kg i.p.) or eltoprazine (1 mg kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones [4]. [1]. Sijbesma H, et al. Eltoprazine, a drug which reduces aggressive behaviour, binds selectively to 5-HT1 receptor sites in the rat brain: an autoradiographic study. Eur J Pharmacol. 1990 Feb 20;177(1-2):55-66. [2]. Joels M, et al. Eltoprazine suppresses hyperpolarizing responses to serotonin in rat hippocampus. J Pharmacol Exp Ther. 1990 Apr;253(1):284-9. [3]. Bezard E, et al. Study of the antidyskinetic effect of eltoprazine in animal models of levodopa-induced dyskinesia. Mov Disord. 2013 Jul;28(8):1088-96. [4]. Rocha B, et al. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31.

Rauwolscine hydrochloride (Isoyohimbine hydrochloride) 是一种高选择性的 α2 adrenergic 受体拮抗剂，Ki=12 nM。

Izuforant (JW1601) (Compound 24) 具有有效的抗炎和止痒活性。 Izuforant 对人血清素3受体 (h5-HT3R) 具有结合亲和力，IC50值为 9.1 μM。它也是组胺 H4 受体 (H4R) 的口服活性拮抗剂，对人 H4R 的IC50值为 36 nM。

8-Gingerol 分离自姜的根状茎，是口服有效的 TRPV1激活剂，EC50值为5.0 µM。8-Gingerol 抑制 COX-2，还能抑制体外 H. pylori 的生长。

Indisetron is a 5-HT(3) and 5-HT(4) receptor antagonist. Indisetron reduces 2-methyl-5-serotonin (HT)-induced bradycardia.

Maprotiline-d3 is intended for use as an internal standard for the quantification of maprotiline by GC- or LC-MS. Maprotiline is a tricyclic antidepressant. It binds to the norepinephrine transporter (NET) and is selective for NET over the serotonin and dopamine transporters. Maprotiline also binds to the serotonin (5-HT) receptor subtype 5-HT2A, as well as histamine H1, muscarinic acetylcholine, α1-adrenergic, and dopamine D2 receptors. In vivo, maprotiline inhibits norepinephrine reuptake in rat brain and peripheral tissues. It reduces isolation-induced aggressive behavior and inhibits electrical foot-shock stimulation-induced belligerence in mice when administered at doses ranging from 3 to 10 mg kg. Maprotiline also reduces aggressive behavior in rhesus monkeys housed in groups. Formulations containing maprotiline have been used in the treatment of depression and anxiety.