Opioid GPCR Family Subtypes and Products

What Are Opioid Receptors?

Opioid receptors are a family of G protein-coupled receptors (GPCRs) comprised of five receptor subtypes: delta, kappa, mu, nociceptin receptor, and zeta. Opioid receptors are found all throughout the brain, spinal cord, and digestive tract. They play a major role in a variety of functions including analgesia, anti-depression, anxiety, euphoria, appetite, and sedation. There are currently a large host of clinical drugs that target the mu receptor for its analgesic effects, such as morphine and naloxone.

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Opioid Receptor Information

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Delta

Kappa

NOP

δ opioid receptor (DOR) inhibits neurotransmitter release by reducing Ca++ currents and increasing K+ conductance. In rats, morphine tolerance is associated with DOR-mediated activation of cortical CCKergic systems. There are indications that some DOR antagonists produce potent antitussive effects and may be considered as candidates of antitussive drugs. In contrast, some DOR agonists have shown antinociceptive, seizuregenic and convulsive properties, implicating a role for the DOR in depression. Early clinical experiments have demonstrated that exogenously administered opioid peptides had antidepressant activity in human patients, suggesting that the receptor may provide a new therapeutic target for treating depression.

κ Opioid Receptor (KOR) is a receptor for dynorphins. KOR inhibits neurotransmitter release by reducing calcium currents and increasing potassium conductance and may play a role in arousal and regulation of autonomic and neuroendocrine functions. Some studies suggest that stimulation of KOR improves memory dysfunctions resulting from the blockade of muscarinic M1 receptors. In addition, KOR agonists attenuate several behavioral responses induced by drugs of abuse, raising the possibility that KOR agonists may be useful for the treatment of dependence on drugs of abuse.

μ opioid receptor (MOR) is a G protein-coupled receptor for β-endorphin. The receptor activation inhibits neurotransmitter release by reducing calcium currents and increasing potassium conductance. MOR mediates positive reinforcement following direct (morphine) or indirect (alcohol, cannabinoids, nicotine) activation. MOR plays a genetic role in the control of gut inflammation. MOR-deficient mice are highly susceptible to colon inflammation, with a 50% mortality rate occurring 3 days after administration of TNBS that induces inflammation. MOR agonists regulate cytokine production and T cell proliferation and might be new therapeutic molecules in inflammatory bowel disease.

NOP, ORL1 or OPRL1 (opioid receptor-like 1 receptor) is also known as nociceptin receptor, orphanin FQ receptor and KOR-3 (kappa 3-related opioid receptor). It is a receptor for the neuropeptide nociceptin/orphanin FQ and has a potential role in modulating a number of brain functions, including instinctive behaviors and emotions. In vivo experiments have demonstrated that nociceptin modulates a variety of biological functions including nociception, food intake, memory processes, cardiovascular and renal functions, spontaneous locomotor activity, gastrointestinal motility, anxiety and neurotransmitter release at peripheral and central sites.

Opioid Cell Lines

Receptor Family	Receptor	Species	Parental	Stable Cell Lines	Division-Arrested Cells	Membranes
Opioid	delta	human	CHO-K1	C1351-1	DC1351-1	MC1351-1
	delta	human	CHO-K1 Gαqi5	CG1351-1	DCG1351-1	MCG1351-1
	delta	human	CHO-K1	CA1351-1	DCA1351-1	MCA1351-1
	delta	rat	CHO dhfr-	C1351	DC1351	MC1351
	kappa	human	CHO-K1	C1352-1a	DC1352-1a	MC1352-1a
	kappa	human	CHO-K1 Gαqi5	CG1352-1	DCG1352-1	MCG1352-1
	kappa	human	CHO-K1	CA1352-1a	DCA1352-1a	MCA1352-1a
	kappa	human	CHO-K1 β-Arrestin2	CA1352BA2-1	DCA1352BA2-1	MCA1352BA2-1
	kappa	human	HEK293T	C1352	DC1352	MC1352
	kappa	rat	CHO dhfr-	C1352-1	DC1352-1	MC1352-1
	kappa	rat	CHO dhfr-	Cr1352-8	DCr1352-8	MCr1352-8
	mu	human	CHO-K1	C1350-1a	DC1350-1a	MC1350-1a
	mu	human	CHO-K1 Gαqi5	CG1350-1a	DCG1350-1a	MCG1350-1a
	mu	human	CHO-K1	CA1350-1a	DCA1350-1a	MCA1350-1a
	mu	rat	CHO dhfr-	Cr1350-1a	DCr1350-1a	MCr1350-1a
	mu Mutant Y150F	human	CHO-K1	C1350-1MT1	DC1350-1MT1	MC1350-1MT1
	mu Mutant Y150A	human	CHO-K1	C1350-1MT2	DC1350-1MT2	MC1350-1MT2
	mu Mutant M153A	human	CHO-K1	C1350-1MT3	DC1350-1MT3	MC1350-1MT3
	mu Mutant H299N	human	CHO-K1	C1350-1MT4	DC1350-1MT4	MC1350-1MT4
	mu Mutant H299A	human	CHO-K1	C1350-1MT5	DC1350-1MT5	MC1350-1MT5
	NOP	human	CHO-K1	C1354-1	DC1354-1	MC1354-1
	NOP	human	CHO-K1 Gαqi5	CG1354-1	DCG1354-1	MCG1354-1
	NOP	human	CHO-K1 β-Arrestin2	CA1354-1	DCA1354-1	MCA1354-1
	NOP	human	HEK293T	C1354a	DC1354a	MC1354a
	NOP	rat	CHO dhfr-	Cr1354	DCr1354	MCr1354