Abstract
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.
Original language | English (US) |
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Pages (from-to) | 5505-5511 |
Number of pages | 7 |
Journal | Journal of medicinal chemistry |
Volume | 46 |
Issue number | 25 |
DOIs | |
State | Published - Dec 4 2003 |