5-ht1 receptor

Pipamperone (McN-JR 3345) 是5-HT2A 受体和D4受体的高亲和力拮抗剂，也是D2受体的低亲和力拮抗剂，pKi 分别为 8.2、8.0 和 6.7。

NEO 376 (SPI-376) 是选择性5-HT1 受体、GABA 受体和多巴胺受体调节剂，可用于精神病的研究。

Rodatristat ethyl (KAR5585) 是一种首新型具有口服活性和有效性的 tryptophan hydroxylase 1 (TPH1) 抑制剂，低浓度下可显著降低 5-hydroxytryptamine (5-HT) 的水平并降低肺动脉高压 (PAH)，

Olanzapine (LY170053) 是一种非典型抗精神病药，目前用于治疗精神分裂症和双相情感障碍。

Perospirone (Lullan) 是具有口服活性的5-HT2A 受体和多巴胺 D2受体的拮抗剂，也是5-HT1A 受体的部分激动剂，Ki 分别为 0.6 、1.4和2.9 nM。它是一种非典型的抗精神病剂，可用于精神分裂症的研究。

Cinanserin is a serotonin 5-HT2 antagonist.

Perospirone hydrochloride (Perospirone HCl) 是非典型的抗精神病剂，可用于精神分裂症的研究。它是可口服的5-HT2A 受体和多巴胺 D2受体的拮抗剂，也是5-HT1A 受体的部分激动剂。

Sumatriptan succinate (GR 43175) 是一种5-HT1受体激动剂，可作用于偏头疼的急性治疗。

Sumatriptan (GR 43175 free base) 是一种可穿过血脑屏障且具有口服活性和高效性的5-羟色胺1（5-HT1） 受体激动剂，具有抗炎活性，对 5-HT1D、5-HT1B 和 5-HT1F 受体具有较高亲和力，可用于急性偏头痛和急性心肌梗死。

Naratriptan 是一种5-HT1受体选择性激动剂，可作用于偏头疼。

Quetiapine (ICI204636) 是5-HT 受体激动剂和多巴胺受体拮抗剂，对人5-HT1A 的 pEC50值为 4.77，对人 D2的 pIC50值为 6.33。它用于治疗精神分裂症，以及治疗与 I 型双相情感障碍相关的急性躁狂发作。它对人 D2、HT1、5-HT2A、5-HT2C 受体具有中高等亲和力，pKi 值为 7.25、5.74、7.54和5.55。

Naratriptan D3 Hydrochloride, the deuterium-labeled form of Naratriptan, is a selective agonist of the 5-HT1 receptor subtype.

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。

Cinitapride (Blaston) 是一种促胃药。它减缓肌肉的活动，以减轻诸如胃酸反流、胃排空延迟和溃疡性消化不良等病症的症状。 Cinitapride 作为 5-HT2 受体的拮抗剂和 5-HT1 和 5-HT4 受体的激动剂。

Cinitapride Hydrogen Tartrate is a gastroprokinetic agent that acts as an antagonist of the 5-HT2 receptors and as an agonist of the 5-HT1 and 5-HT4 receptors

5-Carboxamidotryptamine maleate (5-CT maleate) (5-CT maleate) 是一种 受体激动剂，具有降压和升血糖的作用。

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.

Metergoline (Methergoline) 是多巴胺激动剂和血清素拮抗剂。它是 h5-HT7受体的高亲和力配体，Ki 为 16 nM。它还是可逆神经 Na+通道抑制剂，用于研究季节性情绪障碍、催乳激素调节。

Methiothepin maleate (Metitepine) 是一种 5-HT1、5-HT6、5-HT7 血清素受体拮抗剂，可阻断血清素自身受体。

Sumatriptan (GR 43175) hydrochloride 可用于研究偏头痛，它是一种口服有效的5-HT1受体激动剂。Sumatriptan hydrochloride 对5-HT1D、5-HT1B 和5-HT1A 受体的 Ki 值分别为 17 nM、27 nM 和 100 nM。

Naratriptan hydrochloride (GR-85548A hydrochloride) 是一种5-HT1受体激动剂，有抗偏头疼特性。它还可以通过刺激三叉神经系统感觉神经末梢上的 5-HT1D 1B 受体来发挥其作用，从而减少促炎神经肽的释放。

Isamoltane is a serotonin 5-HT1 Receptor Antagonist

Avitriptan, also known as BMS-180048, is a selective 5-HT1-like receptor agonist. Avitriptan is an effective compound for the treatment of migraine headaches with a prolonged duration of response. Avitriptan Is a Ligand and Agonist of Human Aryl Hydrocarbon Receptor That Induces CYP1A1 in Hepatic and Intestinal Cells.

CP94253 是一种口服有效的5-HT1B选择性激动剂，作用机制为通过与碘氰基吲哚洛尔 (ICP) 竞争性结合5-HT1受体。它与5-HT1B、5-HT1A、5-HT1D、5-HT1C和5-HT2受体结合，Ki值分别为2、89、49、860和1600 nM。在大鼠模型中，CP94253导致饱腹感、厌食、体重减轻和运动亢进。