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.
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH2-Bid into delta-opioid antagonists by N-1-benzimidazole alkylation
GUERRINI, Remo;SALVADORI, Severo;
2005
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.File in questo prodotto:
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