5-ht2c (rat)

Ketanserin (Ketanserinum) 是一种喹唑啉衍生物和 5-羟色胺受体亚型 2 拮抗剂，具有潜在的抗高血压和抗血小板活性。它也浓度依赖性抑制 hERG 电流，IC50为 0.11 μM。

LY 344864 hydrochloride 是选择性的受体激动剂，对5-HT1F 受体具有6 nM(Ki)的亲和力。

Iloperidone (HP 873) 是一种D2 5-HT2受体拮抗剂，是非典型抗精神病药，可治疗精神分裂症。

SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1].in vivo: SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg kg i.p., and 2.0 mg kg p.o. SB 242084 (0.1-1 mg kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].

GR 113808 是一种具有选择性的 5-HT4 receptor 拮抗剂，抑制 5-HT1B，5-HT2A，5-HT2C 和 5-HT3 受体，可减弱多巴胺释放。

Org-12962 是选择性，具有口服活性的 5-HT2C 受体激动剂，pEC50 值为 7.01。 Org-12962 对 5-HT2A 和 5-HT2B 受体也具有很高的作用，pEC50 分别为 6.38 和 6.28。Org-12962 在焦虑大鼠的模型中显示出缓解作用。

ASP-2205，作为一种5-HT2C受体激动剂，具有针对性的激活效果（人5-HT2C受体，EC50=0.85 nM; 大鼠5-HT2C受体，EC50=2.5 nM）。该化合物通过增强通过5-HT2C受体介导的阴部神经尿道闭合反射，有效地用于预防尿失禁。

25B-NBF hydrochloride 是 5-HT2C 受体的高效激动剂，pKi 值在与人类 5-HT2A 受体结合时为 8.57，与大鼠 5-HT2C 受体结合时为 7.73。

Iloperidone hydrochloride is a D(2) 5-HT(2) receptor antagonist. It is also an atypical antipsychotic for the treatment of schizophrenia symptoms.

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.

Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors. It has shown potent activity with IC 50 values of 6.5 nM for rat 5-HT 1A , 0.1 nM for human 5-HT 1A , 15.1 nM for rat D 2 , 17 nM for human D 2 , 6.8 nM for human D 3 , and 2.4 nM for human D 4.2 .

RO1138452 (CAY10441) 是一种选择性和可口服的前列环素受体拮抗剂，pKi 为8.3。它拮抗卡前列环素诱导的人神经母细胞瘤腺苷酸环化酶的激活，以剂量依赖性方式阻断环 AMP 积累，具有镇痛活性。

ANN33840 is a novel selective 5-HT2C agonist with >300-fold functional selectivity over 5-HT2B and >70-fold functional selectivity over 5-HT2A, reducing food intake in an acute rat feeding model.