Volinanserin 是选择性的5-HT2受体拮抗剂，Ki值为 0.36 nM，可用于精神疾病的研究。它对 5-HT2 受体的选择性比 5-HT1c、α-1 肾上腺素能受体和 σ 受体高 300 倍。

Volinanserin (MDL 100907) is a potent and selective antagonist of the serotonin receptor 5-HT2 (Ki: 0.36 nM) and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 adrenergic and sigma receptors.

MDL 100,907 demonstrated low nanomolar or subnanomolar binding in vitro at the 5-HT2A receptor and showed a >100-fold separation from all other receptors measured. MDL 100,907 had subnanomolar potency as a 5-HT2A antagonist in vitro in reversing 5-HT-stimulated inositol phosphate accumulation in NIH 3T3 cells transfected with the rat 5-HT2A receptor [2].

In mice, MDL 100,907 blocked amphetamine-stimulated locomotion at doses that did not significantly affect apomorphine-stimulated climbing behavior. When administered chronically, MDL 100,907 selectively reduced the number of spontaneously active A10 neurons [1]. In vivo, MDL 100,907 potently inhibited 5-methoxy-N, N-dimethyltryptamine-induced head twitches in mice or 5-hydroxytryptophan-induced head twitches in rats. In vivo, functional tests in mice revealed a >500-fold separation between doses that produced 5-HT2A antagonism and doses that produced alpha 1-adrenergic or striatal D2 antagonism [2].

139290-65-6

C22H28FNO3

373.46

氟利色林;MDL100907;M 100907

DMSO:100 mg/mL (267.8 mM)
Ethanol:18 mg/mL (48.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years