orl1 antagonist 1

ORL1 antagonist 1 is an o antagonist of pioid receptor-like 1 (ORL1) (IC50 of 61 nM).

(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist (K(i): cloned human ORL1=1.8 nM). J-113397 inhibited nociceptin orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin orphanin FQ [1].

JTC-801 is a selective opioid receptor-like 1 (ORL1) receptor antagonist with an IC50 of 94 nM and weak inhibitory effects on δ, κ, and μ receptors.

Ac-RYYRIK-NH2 TFA acts as both a potent partial agonist for ORL1 when transfected in CHO cells (K d = 1.5 nM) and an endogenous ligand of ORL1. Moreover, it serves as a specific antagonist that inhibits G protein activation and competitively blocks the stimulation of [35S]-GTPγS binding to G proteins by nociceptin orphanin FQ (noc OFQ) in rat brain membranes and sections [1].

ORL1 antagonist 2 (1B) serves as an antagonist for the opioid receptor-like 1 (ORL1) and is utilized in research on P-glycoprotein (P-gp) [1].