714978-30-0Relevant articles and documents
A bivalent ligand (KMN-21) antagonist for μ/κ heterodimeric opioid receptors
Zhang, Shijun,Yekkirala, Ajay,Tang, Ye,Portoghese, Philip S.
, p. 6978 - 6980 (2009)
In an effort to develop antagonists for κ-μ opioid receptor heterodimers, a series of bivalent ligands 3-6 containing κ- and μ-antagonist pharmacophores were designed and synthesized. Evaluation of the series in HEK-293 cells revealed 4 (KMN-21) to select
A bivalent ligand (KDN-21) reveals spinal δ and κ opioid receptors are organized as heterodimers that give rise to δ1 and δ2 phenotypes. Selective targeting of δ-κ heterodimers
Bhushan, Rashmi G.,Sharma, Shiv K.,Xie, Zhihua,Daniels, David J.,Portoghese, Philip S.
, p. 2969 - 2972 (2007/10/03)
In view of recent pharmacological studies suggesting the existence of δ-κ opioid receptor heterodimers/oligomers in the spinal cord, we have synthesized and evaluated (intrathecally in mice) a series of bivalent ligands (KDN series) containing κ and δ antagonist pharmacophores. Pharmacological and binding data have provided evidence for the bridging of spinal δ-κ receptor heterodimers by KDN-21 and for their identification as δ1 and κ2. The selectivity profile of KDN-21 and the apparent absence of coupled δ 1-κ2 phenotypes in the brain suggest a new approach for targeting receptors.
