A sigma-1 receptor selective analogue of BD1008. A potential substitute for (+)-opioids in sigma receptor binding assays.
A simple, achiral monoamine sigma-1 (sigma1) receptor selective ligand (sigma2Ki/sigma1Ki>2000) is described, which could replace the chiral (+)-pentazocine or dextrallorphan as a sigma1 masking agent in sigma2 binding assays.
Maeda
D Y
DY
Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, USA.
Williams
W
W
Bowen
W D
WD
Coop
A
A
D000701:Analgesics, Opioid / Q000378:metabolism*; D001667:Binding, Competitive; D005021:Ethylamines / Q000378:metabolism* / Q000494:pharmacology; D007700:Kinetics; D007977:Levallorphan / Q000378:metabolism / Q000494:pharmacology; D008024:Ligands; D010423:Pentazocine / Q000378:metabolism / Q000494:pharmacology; D010648:Phenylacetates / Q000138:chemical synthesis / Q000378:metabolism*; D011759:Pyrrolidines / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology; D017480:Receptors, sigma / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity; D000097605:Sigma-1 Receptor
D000701:Analgesics, Opioid; D005021:Ethylamines; D007977:Levallorphan; D008024:Ligands; D010423:Pentazocine; D010648:Phenylacetates; D011759:Pyrrolidines; D017480:Receptors, sigma; D000097605:Sigma-1 Receptor; C106107:sigma-2 receptor; C085527:BD 1008; C044130:dextrallorphan; C404214:AC 915