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Samidorphan (ALKS-33) is a selective opioid antagonist which blocks the μ-opioid receptor, but without blocking δ-opioid or κ-opioid receptors. It has been investigated for the treatment of alcoholism and cocaine addiction,〔(ALK33BUP-101: Safety and Pharmacodynamic Effects of ALKS 33-BUP Administered Alone and When Co-administered With Cocaine )〕 showing similar efficacy to naltrexone but possibly with reduced side effects. However, it has attracted much more attention as part of the combination product ALKS-5461, where samidorphan is combined with the mixed μ-opioid agonist and κ-opioid antagonist opioid modulator buprenorphine, as an antidepressant. Buprenorphine has shown antidepressant effects in some human studies, thought to be because of its antagonist effects at the κ-opioid receptor, but has not been further developed for this application because of its μ-opioid agonist effects and consequent abuse potential. By combining buprenorphine with samidorphan to block the μ-opioid agonist effects, the combination acts more like a selective κ-opioid antagonist, and produces only antidepressant effects, without typical μ-opioid effects being evident.〔(ALKS 5461 drug found to reduce depressive symptoms in Phase 1/2 study )〕〔(Investigational ALKS 5461 Channels ‘Opium Cure’ for Depression )〕 It is also being studied in combination with olanzapine, as ALKS-3831, for use in schizophenia. It is hoped it will be effective while resulting in less weight gain. Phase 2 studies have begun. ==See also== * 8-Carboxamidocyclazocine * Cyprodime * JDTic 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「samidorphan」の詳細全文を読む スポンサード リンク
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