4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective δ-opioid agonists

Add time:08/30/2019    Source:sciencedirect.com

A novel series of 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives has been prepared and their synthesis described herein. In vitro affinities for δ-, μ-, and κ-opioid receptors, as well as the functional activity in the [35S]GTPγS assay are reported. The most potent and selective δ-opioid agonist 18a exhibited a Ki of 18 nM, and was >258-fold and 28-fold selective over μ- and κ-receptors, respectively; the compound is a full agonist with an EC50 value of 14 nM.

We also recommend Trading Suppliers and Manufacturers of 2'-(2-Methylphenylaminocarbonyl)-7'-methylspiro[cyclohexane-1,3'-[3H]indole] (cas 18391-96-3). Pls Click Website Link as below: cas 18391-96-3 suppliers

Prev:Triple ion formation ability of picrate in protophobic aprotic solvents with very low basicity
Next:Research paperDesign, synthesis, and anti-proliferative activity of 1-(4-methoxyphenyl)-12-hydroxymethyl-p-carborane derivatives)