Matches in DBpedia 2016-04 for { ?s ?p "Samidorphan (INN, USAN) (developmental code names ALKS-33, RDC-0313), also known as 3-carboxamido-4-hydroxynaltrexone, is an opioid antagonist that selectively blocks the μ-opioid receptor, without blocking the δ-opioid or κ-opioid receptors. It has been investigated for the treatment of alcoholism and cocaine addiction by its developer, Alkermes, 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.Samidorphan 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 II studies have begun."@en }
Showing triples 1 to 2 of
2
with 100 triples per page.
- Samidorphan abstract "Samidorphan (INN, USAN) (developmental code names ALKS-33, RDC-0313), also known as 3-carboxamido-4-hydroxynaltrexone, is an opioid antagonist that selectively blocks the μ-opioid receptor, without blocking the δ-opioid or κ-opioid receptors. It has been investigated for the treatment of alcoholism and cocaine addiction by its developer, Alkermes, 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.Samidorphan 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 II studies have begun.".
- Q7409428 abstract "Samidorphan (INN, USAN) (developmental code names ALKS-33, RDC-0313), also known as 3-carboxamido-4-hydroxynaltrexone, is an opioid antagonist that selectively blocks the μ-opioid receptor, without blocking the δ-opioid or κ-opioid receptors. It has been investigated for the treatment of alcoholism and cocaine addiction by its developer, Alkermes, 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.Samidorphan 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 II studies have begun.".