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Osemozotan : ウィキペディア英語版
Osemozotan

Osemozotan (MKC-242) is a selective 5-HT1A receptor agonist with some functional selectivity, acting as a full agonist at presynaptic and a partial agonist at postsynaptic 5-HT1A receptors. 5-HT1A receptor stimulation influences the release of various neurotransmitters including serotonin, dopamine, norepinephrine, and acetylcholine.〔Matsuda, Toshio. "Neuropharmacologic Studies on the Brain Serotonin1A Receptor Using the Selective Agonist Osemozotan." ''Biol.Pharm.Bull''. 36.12 (2013): 1871-882.〕 5-HT1A receptors are inhibitory G protein-coupled receptor.〔Saudou F, Hen R. 5-Hydroxytryptamine receptor subtypes in vertebrates and invertebrates. ''Neurochem. Int.'', 25, 503-532 (1994)〕 Osemozotan has antidepressant, anxiolytic, antiobsessional, serenic, and analgesic effects in animal studies,〔Abe, Michikazu, Hiroshi Nakai, Reiko Tabata, Ken-Ichi Saito, and Mitsuo Egawa. "Effect of 5--1,3-benzodioxole HCL (MKC-242), a Novel 5-HT1A-Receptor Agonist, on Aggressive Behavior and Marble Burying Behavior in Mice." ''Jpn. J. Pharmacol.'' 76 (1998): 297-304.〕
,〔 and is used to investigate the role of 5-HT1A receptors in modulating the release of dopamine and serotonin in the brain, and their involvement in addiction to abused stimulants such as cocaine and methamphetamine.
==Pharmacodynamics==
The target of Osemozotan is 5-HT1A receptors. This molecules bind with almost 1000 times greater affinity to 5-HT1A receptors than most other 5-HT, dopamine, or adrenergic receptors.〔 With repeated exposure of Osemozotan at the 5-HT1A receptors, there seems to be no change in the number of receptors, which is not typically seen with pharmaceutical agonists.〔Asano, Shoichi, Toshio Matsuda, Takashi Yoshikawa, Pranee Somboonthum, Hatsue Tasaki, Michikazu Abe, and Akemichi Baba. "Interaction of Orally Administered 5--1,3-benzodioxole (MKC-242) with 5-HT1A Receptors in Rat Brain." Jpn. J. Pharmacol. 74 (1997): 69-75.〕

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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