SB-334867-A: the first selective orexin-1 receptor antagonist
نویسندگان
چکیده
منابع مشابه
The orexin-1 antagonist SB-334867 blocks antipsychotic treatment emergent catalepsy: implications for the treatment of extrapyramidal symptoms.
We have previously shown that the orexin-1 antagonist SB-334867 blocks the electrophysiological effects of haloperidol and olanzapine on the activity of A9 and A10 dopamine neurons. To evaluate if orexin-1 antagonists might block other effects of antipsychotic drugs in animals, we examined the effects of SB-334867 on behavioral, neurochemical, and neuroendocrine effects of antipsychotic drugs. ...
متن کاملDisposition and Metabolism of [C]SB-649868, an Orexin 1 and 2 Receptor Antagonist, in Humans
N-[[(2S)-1-[[5-(4-fluorophenyl)-2-methyl-4-thiazolyl]carbonyl]-2piperidinyl]methyl]-4-benzofurancarboxamide (SB-649868) is a novel orexin 1 and 2 receptor antagonist under development for insomnia treatment. The disposition of [C]SB-649868 was determined in eight healthy male subjects using an open-label study design after a single oral dose of 30 mg. Blood, urine, and feces were collected at f...
متن کاملDisposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans.
N-[[(2S)-1-[[5-(4-fluorophenyl)-2-methyl-4-thiazolyl]carbonyl]-2-piperidinyl]methyl]-4-benzofurancarboxamide (SB-649868) is a novel orexin 1 and 2 receptor antagonist under development for insomnia treatment. The disposition of [(14)C]SB-649868 was determined in eight healthy male subjects using an open-label study design after a single oral dose of 30 mg. Blood, urine, and feces were collected...
متن کاملAdministration of orexin receptor 1 antagonist into the rostral ventromedial medulla increased swim stress-induced antinociception in rat
Objective(s): Intracerebroventricular injection of orexin-A (hypocretin-1) antagonist has been shown to inhibit stress-induced analgesia. However the locations of central sites that may mediate these effects have not been totally demonstrated. This study was performed to investigate the role of rostral ventromedial medulla (RVM) orexin receptor 1 in stress-induced analgesia (SIA). Materials and...
متن کاملIntra-paragigantocellularis lateralis injection of orexin-A has an antinociceptive effect on hot plate and formalin tests in rat.
In the present study, the effect of orexin-A (ORXA) microinjection into the paragigantocellularis lateralis (LPGI) on nociceptive behaviors, using hot-plate and formalin tests as thermal and chemical models of pain in rat, was examined. Also, we determined whether the pretreatment with SB-334867, a selective OX1-receptor antagonist, would prevent the antinociceptive effect of orexin-A. ORXA (0....
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2001
ISSN: 0007-1188
DOI: 10.1038/sj.bjp.0703953