62 products were found matching "K04214"!

Recombinant CHO-K1 cells stably overexpress human opioid receptor kappa 1 (OPRK1) on the surface and contain high levels of G protein Galphai to couple with the receptor in downstream signaling pathways.

Aticaprant is a kappa-opioid receptor (KOR) antagonist (Ki = 0.807 nM). It is selective for KOR over the µ- and delta-opioid receptors (Kis = 24 and 155 nM, respectively). Aticaprant reverses U-69593-induced decreases in nocifensive behavior in the formalin test in rats (ED50 = 0.4 mg/kg). It also reverses...

Salvinorin B (Cay-23582) is an analytical reference standard categorized as a diterpene. Salvinorin B is a presumptive metabolite of salvinorin A (Cay-38208, Cay-11487). It has been found in S. divinorum, a plant with hallucinogenic properties. This product is intended for research and forensic applications.Formal...

Nalfurafine (Cay-23186) is an analytical reference standard categorized as an opioid. Naflurafine decreases ethanol consumption in male mice and increases ethanol consumption in female mice. It is regulated as a Schedule II compound in the United States. This product is intended for research and forensic...

0.5 mg/ml in 1X TBS, pH7.3, with 0.5% BSA (US sourced) and 0.02% sodium azide. Additional name(s) for this target protein: KOR, OPRK, OPRK1 Protein function: G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also...

SCH 202676 is a reversible inhibitor of both agonist and antagonist binding to diverse G protein-coupled receptors (GPCRs). It blocks the binding of radiolabeled ligands to human opioid, adrenergic, muscarinic, dopaminergic, adenosine, and purinergic receptors. It displays IC50 values of 0.1 to 1.8 µM for modulating...

Salvinorin B mesylate (Mesyl Sal B) is a selective kappa-opioid receptor agonist that is more potent than salvinorin A (Cay-11487) in CHO cells transfected with the human kappa-opioid receptor (EC50s = 30 and 40 nM, respectively). It is a mesylated version of salvinorin B (Cay-11488) and is highly selective for...

Salvinorin A carbamate is a potent kappa-opioid receptor (KOR) full agonist that is almost as potent as salvinorin A (Cay-11487) with EC50 values of 6.2 and 4.5 nM, respectively, for activation of the human KOR to enhance binding of [35S]GTPgammaS. The addition of a carbamate group to salvinorin A increases...

Asimadoline is a potent kappa-opioid receptor (KOR) agonist (IC50s = 5.6 and 1.2 nM for guinea pig and human receptors, respectively). It is 501- and 498-fold selective for kappa-opioid over µ- and delta-opioid receptors, respectively. Asimadoline is spasmolytic in isolated rat duodenum (IC50 = 4.2 µM) and inhibits...

GNTI is a kappa-opioid receptor antagonist (Ki = 0.18 nM). It is selective for kappa-opioid receptors over µ- and delta-opioid receptors in radioligand binding assays (Kis = 36.9 and 70 nM, respectively). GNTI inhibits agonist-induced [35S]GTPgammaS binding in CHO cells expressing human kappa-opioid receptors (pA2 =...

Trimebutine is an opioid receptor agonist. It binds to µ-, delta-, and kappa-opioid receptors with Ki values of 0.34, 0.5, and 0.58 µM, respectively, in canine myenteric plexus synaptosomes. Trimebutine inhibits twitch contraction and acetylcholine (ACh) release induced by low-frequency electrical stimulation in...

LY2795050 is a kappa-opioid receptor antagonist (Ki = 0.722 nM). It is selective for kappa-opioid receptors over µ- and delta-opioid receptors (Kis = 25.8 and 153 nM, respectively). LY2795050 (0.1 mg/kg, i.p.) reduces immobility time in the forced swim test, as well as reduces salvinorin A-induced decreases in...