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Abstract
N1-Alkylation of 1H-benzimidizole of the ä agonist
H-Dmt-Tic-NH-CH2-Bid with hydrophobic, aromatic, olefinic,
acid, ethyl ester, or amide (1-6) became ä antagonists (pA2 )
8.52-10.14). ä- and í-Opioid receptor affinities were high (Kiä
) 0.12-0.36 nM and Kií ) 0.44-1.42 nM). Only ä antagonism
(pA2 ) 8.52-10.14) was observed; í agonism (IC50 ) 30-450
nM) was not correlated with changes in alkylating agent or ä
antagonism, and some compounds yielded mixed ä antagonism/
í agonism
