Add time:07/21/2019         Source:sciencedirect.com

Analogues of 3,4-dimethyl-4-(3-hydroxyphenyl)piperidines are high affinity inverse agonists for μ-, δ- and κ-opioid receptors. To characterize inverse agonist binding, we synthesized a high specific activity radioligand from this series, [3H]LY515300 (3-[1-((3-cyclohexyl-[3,4-3H2])-3(R,S)-hydroxypropyl)-3(R),4(R)-dimethylpiperidin-4-yl]phenol). In membranes expressing cloned human opioid receptors, [3H]LY515300 binding was saturable and exhibited low nonspecific binding. [3H]LY515300 bound with high affinity to the μ- (Kd=0.07 nM), δ- (Kd=0.92 nM) and κ-(Kd=0.45 nM) opioid receptors. High affinity [3H]LY515300 binding to all opioid receptors was Na+-dependent, a characteristic of inverse agonists. Displacement by standard opioid compounds yielded Ki values consistent with their known opioid receptor affinities. Autoradiographic localization of specific [3H]LY515300 binding in rat and guinea pig brain was high in areas known to express high levels of opioid (particularly μ-opioid receptor) binding sites including the caudate, nucleus accumbens, and nucleus tractus solitarius. Thus, [3H]LY515300 is the first radiolabeled opioid receptor inverse agonist useful for the study of opioid receptors in cell lines and native tissues.

We also recommend Trading Suppliers and Manufacturers of 4-[2-ethyl-1-(4-hydroxyphenyl)but-1-enyl]phenol (cas 16174-47-3). Pls Click Website Link as below: cas 16174-47-3 suppliers