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71670 AM251
(CAS 183232-66-8)
AM251 Workbook Links
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Chemical structure definitions are available for many Cayman products. See Chemical Structure Database for details.
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SR 141716A is a biarylpyrazole compound which has been considered for many years as the prototypical cannabinoid (CB) receptor antagonist.1 Some very close structural relatives of SR 141716A were recently prepared and tested for their ability to act as antagonists of the CB1 receptor.2 AM251 is one of these analogs, wherein 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 compound to SR 141716A, which has a Ki value of 11.5 nM. However AM251 is about two-fold more selective for the CB1 receptor when compared to SR 141716A.2
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1
Rinaldi-Carmona, M., Barth, F., Héaulme, M., et al. SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 350 240-244 (1994).
2
Lan, R., Liu, Q., Fan, P., et al. Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists. J Med Chem 42 769-776 (1999).
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Pricing updated 2010-02-09.
Prices are subject to change without notice.
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Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.
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