spiperone

Spiperone (Spiropitan) 是多巴胺 D2、血清素5-HT1A 和血清素5-HT2A 拮抗剂。它是广泛使用的药理学工具。它具有研究神经系统疾病的潜力。

5-HT2A serotonin and selective D2-like dopamine receptor antagonist

ligand for the D2 receptor

Fluspiperone is an antipsychotic agent.

KML-010是spiperone的衍生物。与spiperone相比，KML-010对5-HT(2A)受体的亲和力略低，但对5-HT(2C)和5-HT(1A)受体几乎不表现出亲和力，并且对多巴胺D2受体的亲和力显著降低。通过将spiperone的N(1)-苯基环改为KML-010中的甲基，其结合特性发生变化，从而可能提供更具选择性的药理学特征，以针对特定的受体。

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.

AHR-5645B free base is a substituted benzamide which has been shown to inhibit 3H-spiperone binding to bovine anterior pituitary membranes.

Cyclindole is an antipsychotic with a tricyclic structure that was never marketed. It displaces spiperone binding in vitro and elevates dopamine levels in the striatum, indicating it acts as a D₂ receptor antagonist.

AHR-5645B fumarate is a substituted benzamide that has been shown to inhibit 3H-spiperone binding to bovine anterior pituitary membranes.