NI-Alkylation of 1H-benzimidizole of the delta agonist H-Dmt-Tic-NH-CH2-Bid with hydrophobic, aromatic, olefinic, acid, ethyl ester, or amide (1-6) became delta antagonists (pA(2) = 8.52-10.14). delta- and mu-Opioid receptor affinities were high (K-i delta = 0.12-0.36 nM and K-i mu = 0.44-1.42 nM). Only delta antagonism (pA(2) = 8.52-10.14) was observed; mu agonism (IC50 = 30-450 nM) was not correlated with changes in alkylating agent or delta antagonism, and some compounds yielded mixed delta antagonism/gamma agonism.
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-Bid into delta-opioid antagonist by N(1)-Benzimidazole Alkylation / Balboni, G.; Guerrini, R.; Salvadori, S.; Negri, Lucia; Giannini, Elisa; Bryant, S. D.; Jinsmaa, Y.; Lazarus, L. H.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 48:(2005), pp. 8112-8114. [10.1021/jm058259l]
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-Bid into delta-opioid antagonist by N(1)-Benzimidazole Alkylation.
NEGRI, Lucia;GIANNINI, Elisa;
2005
Abstract
NI-Alkylation of 1H-benzimidizole of the delta agonist H-Dmt-Tic-NH-CH2-Bid with hydrophobic, aromatic, olefinic, acid, ethyl ester, or amide (1-6) became delta antagonists (pA(2) = 8.52-10.14). delta- and mu-Opioid receptor affinities were high (K-i delta = 0.12-0.36 nM and K-i mu = 0.44-1.42 nM). Only delta antagonism (pA(2) = 8.52-10.14) was observed; mu agonism (IC50 = 30-450 nM) was not correlated with changes in alkylating agent or delta antagonism, and some compounds yielded mixed delta antagonism/gamma agonism.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
