A Bivalent Ligand (KDAN-18) Containing
δ-Antagonist and κ-Agonist
Pharmacophores Bridges δ<sub>2</sub> and κ<sub>1</sub>
Opioid Receptor Phenotypes<sup>†</sup>
David J. Daniels
Amol Kulkarni
Zhihua Xie
Rashmi G. Bhushan
Philip S. Portoghese
10.1021/jm034234f.s001
https://acs.figshare.com/articles/journal_contribution/A_Bivalent_Ligand_KDAN_18_Containing_Antagonist_and_Agonist_Pharmacophores_Bridges_sub_2_sub_and_sub_1_sub_Opioid_Receptor_Phenotypes_sup_sup_/3294505
To characterize δ- and κ-opioid receptor phenotypes, bivalent ligands (KDAN series) containing δ-antagonist
(naltrindole) and <i>κ</i><sub>1</sub>-agonist (ICI-199,441) pharmacophores
were synthesized and evaluated by the intrathecal route using
the mouse tail-flick assay and binding studies. The data have
suggested that KDAN-18 (<b>2</b>) bridges phenotypic δ<sub>2</sub>- and κ<sub>1</sub>-receptors. A conceptual model is presented to explain the
organizational differences between the opioid receptors that
give rise to the phenotypes (δ<sub>1</sub>, δ<sub>2</sub>, κ<sub>1</sub>, κ<sub>2</sub>).
2005-03-24 00:00:00
opioid
receptor
κ 1
phenotype
KDAN
ICI
bridges phenotypic δ 2