Journal
EUROPEAN JOURNAL OF PHARMACOLOGY
Volume 396, Issue 1, Pages 49-52Publisher
ELSEVIER
DOI: 10.1016/S0014-2999(00)00208-9
Keywords
norbinaltorphimine; binding; kappa-opioid receptor
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5'-Guanidinonaltrindole (GNTI) possesses 5-fold greater opioid antagonist potency (K-e = 0.04 nM) and an order of magnitude greater selectivity (selectivity ratios > 500) than the prototypical kappa-opioid receptor antagonist, norbinaltorphimine, in smooth muscle preparations. Binding and functional studies conducted on cloned human opioid receptors expressed in Chinese hamster ovarian (CHO) cells afforded pA(2) values that were comparable to the smooth muscle data. In view of the high selectivity and potency of GNTI, it is a potentially valuable pharmacological tool for opioid research. (C) 2000 Elsevier Science B.V. All rights reserved.
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