human 5-ht2a receptor

Wf-516 is a 5-HT reuptake inhibitor (Kis: 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively), and with potent antidepressant activity.

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。

SB 243213 是一种可口服且具有选择性的 5-HT2C 受体拮抗剂。SB 243213 具有抗焦虑抗抑郁活性，可用于精神分裂症和运动障碍。

Ziprasidone hydrochloride monohydrate (CP 88059) 是一种联合 5-HT（5-羟色胺）和多巴胺受体拮抗剂，具有抗精神病活性的强效作用。它也是去甲肾上腺素再摄取抑制剂。

Ziprasidone hydrochloride (CP-88059 hydrochloride) 是一种联合 5-HT（5-羟色胺）和多巴胺受体拮抗剂，具有抗精神病活性的强效作用。它也是去甲肾上腺素再摄取抑制剂。

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。

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。

Brexpiprazole (OPC-34712) 是人5-HT1A 和多巴胺受体的部分激动剂，Ki 分别为0.12 和 0.3 nM。它也是5-HT2A 受体的拮抗剂，Ki 为 0.47 nM，可作为非典型抗精神病药。

Ziprasidone (Geodon) 是一种联合的 5-HT(5-羟色胺)和多巴胺受体拮抗剂，具有强大的抗精神病活性。它是去甲肾上腺素再摄取抑制剂，对大鼠和人的5-HT1A，5-HT2A 和多巴胺 D2 受体有很高的亲和力。

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].

DREADD agonist 21 是一种人毒蕈碱乙酰胆碱 M3 受体激动剂，EC50为 1.7 nM。

CP-809101 hydrochloride 是选择性 5-HT2C 受体激动剂，对于人类 5-HT2C 5-HT2B 5-HT2A 受体。

SB 243213 hydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8).It has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

SB 243213 dihydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor).

Fananserin 是一种有效的、特异性的、口服活性的 5-HT2 拮抗剂（大鼠 5-HT2A 的 Ki = 0.37 nM）。 Fananserin 是人 D4 受体的拮抗剂 (Ki = 2.93 nM)。

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。

AL 34662 是一种具有选择性和高效性的 5-HT2A 受体激动剂，对大鼠和人 5-HT2 受体的IC50 分别为 0.77 nM 和 1.5 nM。AL 34662 还是一种亲和力较低的 α-1D 肾上腺素能激动剂，EC50 值为 0.4 μM。AL 34662 可用于降低眼压。

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。

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

LY 344864 是一种特异性受体激动剂，有对克隆 5-HT1F 受体的亲和力，Ki 为6 nM。

RS 64459-193 has a high affinity for the 5-HT1A binding site.

Iloperidone metabolite P95 is a metabolite of the atypical antipsychotic iloperidone . It binds to the serotonin (5-HT) receptor subtype 5-HT2A and α1-, α2B-, and α2C-adrenergic receptors with mean Ki values of 7.08, 21.38, 83.18, and 47.86 nM, respectively, but does not cross the blood-brain barrier.

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。