55 products were found matching "K04213"!

Recombinant CHO-K1 cells stably overexpress human opioid receptor delta 1 (OPRD1) on the surface and contain high levels of G protein Galphai to couple with the receptor in downstream signaling pathways.

DPDPE is a synthetic enkephalin peptide and an agonist of delta1-opioid receptors (Ki = 2.7 nM for the rat receptors). It is selective for delta-opioid receptors over µ- and kappa-opioid receptors (Kis = 713 and >1,500 nM, respectively, for the rat receptors). In vivo, DPDPE (4.5 nmol i.c.v.) increases the latency...

Naltriben is an inverse agonist of delta2-opioid receptors (Ki = 0.013 nM in CHO-DG44 cells expressing the mouse receptor). It is selective for delta2-opioid receptors over kappa- and µ-opioid receptors (Kis = 13 and 12 nM in PC12 and COS-7 cells expressing the mouse and rat receptors, respectively). Naltriben (1...

SNC 80 is a selective nonpeptide agonist of the delta-opioid receptor (Ki = 0.18 nM, IC50 = 2.73 nM) that is over 2,000-fold less effective at the µ-opioid receptor. It effectively activates µ/delta receptor heteromers (EC50 = 52.8 nM) but not kappa/delta or µ/kappa heteromers. SNC 80 has antinociceptive as well as...

BNTX is a delta1-opioid receptor antagonist (Ki = 0.1 nM). It is selective for the delta1-opioid receptor over the delta2-, µ-, and kappa-opioid receptors (Kis = 10.8, 13.3, and 58.6 nM, respectively). BNTX (1 and 10 µM) decreases proliferation of primary mouse splenic B cells and the production of IL-2 and IL-4 by...

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...

The µ-opioid receptor (OPRM1) is the primary site of action for morphine and other opioids associated with the treatment of pain. The occupancy of delta-opioid receptors (OPRD1) by antagonists has been shown to enhance OPRM1 binding and signaling activity. Because heteromerization of OPRM1 and OPRD1 is thought to be...

BMS 986187 is a positive allosteric modulator of delta-opioid receptors. In the presence of the endogenous delta-opioid receptor agonist leu-enkephalin, BMS 986187 has an average EC50 value of 30 nM for beta-arrestin recruitment, but has little to no activity in the absence of an agonist. It is 100-fold selective...

Highly selective and potent non-peptide delta-opioid receptor agonist, Mediates downregulation of the delta-opioid receptor, Shows antidepressant-like effects, Modulates voltage-dependent sodium channels, Antinociceptive, Activates ATP-sensitive K channels, Enhances amphetamine-mediated dopamine efflux.

BMS 986188 is a positive allosteric modulator of delta-opioid receptors, with an EC50 value of 0.05 µM in a beta-arrestin recruitment assay in the presence, but not absence, of the opioid receptor agonist leu-enkephalin (Cay-23283). It is selective for delta- over µ-opioid receptors (EC50 = >10 µM) in the presence...

Leu-Enkephalin is an endogenous neuropeptide involved in nociception and an agonist of delta- and µ-opioid receptors (Kis = 4.0 and 3.4 nM, respectively). It is selective for delta- and µ- over kappa-opioid receptors (Ki = >1,000 nM). Leu-Enkephalin is a cleavage product of proenkephalin, which is found primarily in...

Protein function: G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as...