AM-251 (drug)
http://dbpedia.org/resource/AM-251_(drug) an entity of type: Thing
AM251 – organiczny związek chemiczny z grupy kannabinoidów, antagonista receptorów kannabinoidowych. Pod względem farmakologicznym i strukturalnym jest podobne do rimonabantu.
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AM-251 is an inverse agonist at the CB1 cannabinoid receptor. AM-251 is structurally very close to rimonabant; both are cannabinoid receptor antagonists. In AM-251, the p-chloro group attached to the phenyl substituent at C-5 of the pyrazole ring is replaced with a p-iodo group. The resulting compound exhibits slightly better binding affinity for the CB1 receptor (with a Ki value of 7.5 nM) than rimonabant, which has a Ki value of 11.5 nM, AM-251 is, however, about two-fold more selective for the CB1 receptor when compared to rimonabant. Like rimonabant, it is additionally a μ-opioid receptor antagonist that attenuates analgesic effects.
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AM-251 (drug)
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AM251
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AM-251
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AM-251 is an inverse agonist at the CB1 cannabinoid receptor. AM-251 is structurally very close to rimonabant; both are cannabinoid receptor antagonists. In AM-251, the p-chloro group attached to the phenyl substituent at C-5 of the pyrazole ring is replaced with a p-iodo group. The resulting compound exhibits slightly better binding affinity for the CB1 receptor (with a Ki value of 7.5 nM) than rimonabant, which has a Ki value of 11.5 nM, AM-251 is, however, about two-fold more selective for the CB1 receptor when compared to rimonabant. Like rimonabant, it is additionally a μ-opioid receptor antagonist that attenuates analgesic effects. AM251 has shown an in vitro antimelanoma activity against pancreatic and colon cancer cells.
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AM251 – organiczny związek chemiczny z grupy kannabinoidów, antagonista receptorów kannabinoidowych. Pod względem farmakologicznym i strukturalnym jest podobne do rimonabantu.
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