Selective cyclized peptide κ-opioid receptor antagonist - in vivo pharmacology

Modulating the GPCR k-opioid receptor is a promising strategy for treating CNS disorders, where the receptor antagonism is associated with beneficial effects for the treatment of mood and psychiatric diseases, and drug addictive disorders. Behavioral investigations in mice established the in vivo k-opioid receptor antagonist properties of CSD-CH2(1,8)-NH2 after subcutaneous administration in mice based on its ability to reverse the antinociceptive effects of the prototypical k-opioid agonist, U50,488, in a model of acute thermal nociception (the radiant heat tail-flick assay) and to prevent sedation/motor impairment produced by U50,488 in the rotarod test. CSD-CH2(1,8)-NH2 had in vivo antagonist activity by modulating k-opioid receptor function in the CNS.

The dataset includes experimental in vivo pharmacological data on CSD-CH2(1,8)-NH2, a selective cyclized peptide κ-opioid receptor antagonist.