5-ht2a antagonist 1

5-HT2A antagonist 1 is a 5-HT2A antagonist. It may be useful in the treatment of gastrointestinal disorders circulatory disorders.

LE 300 是选择性多巴胺 D1 样受体拮抗剂，作用于人多巴胺 D1 和 D5 受体的Kis 分别为 1.9 nM 和 7.5 nM。在大鼠尾动脉实验中，它作用于5-HT2A 受体的pA2 为 8.32。

Perphenazine dihydrochloride 是一种具有口服活性和高效性的多巴胺受体和组胺-1 受体拮抗剂,抑制 D2、D3 和 5-HT2A。Perphenazine dihydrochloride 抑制癌细胞增殖，并诱导细胞凋亡，可用于研究精神分裂和宫内膜癌。

Sarpogrelate hydrochloride (MCI-9042) 是一种选择性5-HT2R 拮抗剂，可用于研究与血栓形成有关的血管疾病，对 5-HT2A、5-HT2B 和 5-HT2C 受体的pKi 值分别为 8.52、6.57 和 7.43。

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].

Flibanserin, a compound identified as BIMT-17, acts as a complete agonist at the serotonin 5-HT1A receptor, with a binding affinity (Ki) of 1 nM, while functioning as an antagonist at the 5-HT2A receptor with a 49 nM affinity. Flibanserin D4 represents a deuterium-labeled version of Flibanserin.

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。

D3 5-HT receptor modulator-1 (compound 5i) 是一种具有选择性抑制多巴胺D3受体和5-HT2A受体的拮抗剂，同时也是部分激动5-HT1A受体的化合物。该化合物对多巴胺D3、5-HT2A和5-HT1A受体的Ki值分别为4.5 nM、11.9 nM和15.3 nM。相比之下，它对多巴胺D2受体、5-HT2C受体和hERG通道的亲和力较低，具有非典型抗精神病特性。

BGC20-761 是一种选择性的5-HT6和多巴胺受体 (dopamine receptor) 拮抗剂，对人 5-HT6，5-HT2A，D2 受体的Ki 值分别为 20，69，和 140 nM。BGC20-761 可增强长期记忆。BGC20-761 具有作为抗精神病药物的潜在效用。

Cyproheptadine 是一种有效的口服活性5-HT2A 受体拮抗剂。Cyproheptadine 具有抗抑郁和抗血清素作用。Cyproheptadine 还具有抗血小板和血栓保护活性，可用于研究血栓栓塞性疾病。

5-HT6 5-HT2A receptor ligand-1 (compound 33) is a dual antagonist for the 5-HT6 and 5-HT2A receptors. It exhibits a K i value of 2 nM and 11 nM for the respective receptors. This compound holds promise for research in neurological and psychiatric disorders [1].

5-HT6 5-HT2A receptor ligand-2 (化合物 42) 是一种可透过血脑屏障的5-HT6 5-HT2A 的双拮抗剂 ,Ki 值分别为 25 nM 和 32 nM。5-HT6 5-HT2A receptor ligand-2 具有促认知特性。

5-HT6 5-HT2AR antagonist-1 is a powerful and effective compound that acts as a dual antagonist for both the 5-HT6 and 5-HT2A receptors. It exhibits high potency with K i values of 11 nM and 39 nM for the respective receptors [1].

Flibanserin (BIMT-17; BIMT-17BS) hydrochloride 是一种口服具有活力的 5-羟色胺的 5-HT1A 受体激动剂 (Ki: 1 nM) 和 5-HT2A (Ki: 49 nM) 受体拮抗剂。Flibanserin hydrochloride 同时可以结合多巴胺 D4 受体 (Ki: 4-24 nM)。Flibanserin hydrochloride 具有抗抑郁和抗焦虑的效果，能够用于性欲减退 (HSDD) 的研究。

Zicronapine (Lu 31-130) fumarate 是抗精神病药，主要通过拮抗多巴胺D1 D2受体和5-HT2A受体发挥作用，在动物模型中显示出显著的前认知效果，展现出治疗多种神经和精神疾病的可能性。

R-96544 是一种具有口服活性的 5-HT2A 受体拮抗剂，可抑制体外血小板聚集。

5-HT2A antagonist 2 is an orally active, selective 5HT2A antagonist with an IC50 of 14 nM. It exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 [1].

Sarpogrelate-d3 HCl 是 Sarpogrelate HCl 的氘代化合物。Sarpogrelate HCl 的 CAS 号为 135159-51-2。Sarpogrelate hydrochloride 是一种选择性5-HT2R拮抗剂，可用于研究与血栓形成有关的血管疾病，对 5-HT2A、5-HT2B 和 5-HT2C 受体的pKi值分别为 8.52、6.57 和 7.43。