KOR agonist 6 is a KOR agonist with a Ki value of 0.25 pM. In CHO cells, it exhibits agonistic activity on MOR and DOR and inhibits forskolin-stimulated cAMP accumulation. The compound stimulates KOR-mediated [35S]GTPgammaS binding in HEK293 cells expressing KOR and effectively suppresses cAMP accumulation as a potent agonist, showing lower beta-arrestin recruitment efficacy. Additionally, KOR agonist 6 demonstrates analgesic effects in mice and can be employed in the study of analgesics with reduced central nervous system (CNS) side effects.
Target:
Opioid Receptor
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