5-ht-3 antagonist 3

5-HT3 antagonist 3 是一种高亲和力的 5-HT3 受体拮抗剂。5-HT3 antagonist 3 结合到大鼠脑皮质膜中的 5-HT3 受体，Ki 为 0.25 nM。

Litoxetine HCl 是一种选择性5-羟色胺（5-HT）再摄取抑制剂（SSRI）和混合5-羟色胺拮抗剂，可用于治疗尿失禁。Litoxetine HCl 在没有抗毒蕈碱特性的浓度下（10 nM-1 microM）引起大鼠离体食道肌肉粘膜的浓度依赖性松弛，使卡巴胆碱张力降低达37%,更高浓度的Litoxetine HCl（3微摩-300微摩）与明显的松弛有关，直至取消卡巴胆碱张力。以前在离体豚鼠肠道中证明的利托西汀的抗心律失常活性，在浓度大于1 microM 时在大鼠离体食道肌肉粘膜中发挥了作用。 Litoxetine HCl 的5-HT 释放作用可以解释利托西汀对未处理的大鼠组织中的5-HT 诱导的松弛的效力，这种效力被pCPA 处理所逆转。

PRX-07034 hydrochloride 是一种有效的高度选择性5-HT6受体拮抗剂，Ki 为 4-8 nM，IC50为 19 nM，可用于增强工作记忆和认知灵活性的研究。

5-HT3 antagonist 5 是喹喔啉 -2- 甲酰胺化合物，是一种5-HT3受体拮抗剂。5-HT3 antagonist 5 对5-HT3激动剂和2-甲基-5-HT 也具有拮抗作用，并在小鼠中表现出抗抑郁作用。

5-HT3 antagonist 1 is a potent and selective antagonist of 5-HT3 receptor.

5-HT3 antagonist 2 is an antagonist of 5-HT3 receptor.

Ensaculin is a NMDA antagonist and a 5HT1A agonist potentially for the treatment of Alzheimer's disease (AD). Ensaculin showed memory-enhancing effects in paradigms of passive and conditioned avoidance in both normal and artificially amnesic rodents. It e

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

SDZ-216525, a 5-HT1A receptor antagonist, inhibits the tracheal contractions induced both by NKA (10 nM-3 microM) and 5-HT (10 nM-10 microM) (n=4-10).

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.

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

Dopamine D3 受体激动剂13a是一种Dopamine D3 受体激动剂。该化合物选择性地与Dopamine D3 受体结合，相较于Dopamine D1、D2和D4受体(Kis = 0.14、4,600、2.85和756 nM，分别)具有更高的亲和力，并且还能与血清素(5-HT)受体亚型5-HT1A、5-HT2A、5-HT2B和5-HT2C(Kis = 6、54、1.47和252 nM，分别)结合；然而，它是Dopamine D2受体的部分激动剂(EC50 = 2.26 nM，在G蛋白招募分析中)并且作为Dopamine D3受体的拮抗剂(IC50 = 4.62 nM)。在大鼠身上，当剂量为3 mg kg时，Dopamine D3 受体激动剂13a能减少可卡因自我给药。

Lerisetron 是5-HT3拮抗剂，与 5-HT3受体具有高亲和力(pKi:9.2)。它对尿烷麻醉大鼠的 5-HT 引发的反射性心率过缓具有抑制作用。

GR65630是一种高效且具有选择性的5-羟色胺（5-HT）3型受体拮抗剂。该化合物常用于研究5-HT3受体在多个脑区的分布及其在中枢神经系统的潜在功能。通过使用GR65630及其同位素标记的[3H]GR65630，研究人员能够探索受体的分布情况、密度和亲和性。