641611-38-3Relevant academic research and scientific papers
Guanidino N-Substituted and N,N-Disubstituted Derivatives of the κ-Opioid Antagonist GNTI
Black, Shannon L.,Chauvignac, Cedric,Grundt, Peter,Miller, Carl N.,Wood, Susan,Traynor, John R.,Lewis, John W.,Husbands, Stephen M.
, p. 5505 - 5511 (2007/10/03)
Derivatives of the highly selective κ-opioid receptor antagonist GNTI (2a) have been prepared. Binding and functional studies conducted on cloned human opioid receptors expressed in Chinese hamster ovarian (CHO) cells suggested that adding a benzyl or a substituted benzyl group to the guanidino moiety led, in general, to a retention of high κ-affinity and antagonist potency. Disubstitution of the guanidino moiety led to reduced κ-selectivity.
