Ontology highlight
ABSTRACT:
SUBMITTER: Weltrowska G
PROVIDER: S-EPMC2848705 | biostudies-literature | 2010 Apr
REPOSITORIES: biostudies-literature
Weltrowska Grazyna G Chung Nga N NN Lemieux Carole C Guo Jianxin J Lu Yixin Y Wilkes Brian C BC Schiller Peter W PW
Journal of medicinal chemistry 20100401 7
There is evidence to indicate that the Asp residue in the third transmembrane helix (TMH) of opioid receptors forms a salt bridge with the positively charged nitrogen of endogenous and exogenous opioid ligands. To further examine the role of this electrostatic interaction in receptor binding and activation, we synthesized "carba"-analogues of a published fentanyl analogue containing a 3-(guanidinomethyl)-benzyl group in place of the phenyl moiety attached to the ethylamido group (C. Dardonville ...[more]