ZYKR1, a novel, potent, and peripherally selective kappa opioid receptor agonist reduces visceral pain and pruritus in animal models

Autor:	Mukul R. Jain, Rakesh B. Patel, Kanaiyalal D. Prajapati, Purvi Vyas, Debdutta Bandyopadhyay, Vijay Prajapati, Rajesh Bahekar, Prakash N. Patel, Harish M. Kawade, Dadasaheb M. Kokare, Vishwanath Pawar, Ranjit Desai
Rok vydání:	2021
Předmět:	Pharmacology Analgesics Opioid Male Analgesics Mice Pruritus Receptors Opioid kappa Models Animal Receptors Opioid mu Animals Visceral Pain Rats
Zdroj:	European journal of pharmacology. 924
ISSN:	1879-0712
Popis:	Opioid receptor agonists are effective analgesic agents. Central activation of the mu and/or kappa opioid receptors (KOR) is associated with CNS side effects, which limits their effectiveness. Recent studies indicated that peripherally restricted, selective KOR agonists were potent analgesics and devoid of CNS-related side effects. To confirm this hypothesis, we designed a novel, potent, and peripherally restricted KOR-selective agonist, ZYKR1. The analgesic efficacy, brain penetration and safety of ZYKR1 were assessed in pre-clinical models. ZYKR1 showed KOR agonistic activity in the cAMP assay, with an EC
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0ecc752becf307607600d77a07d8345 https://pubmed.ncbi.nlm.nih.gov/35443192 Zobrazit plný text záznamu Full Text from ScienceDirect