μ Opioid Receptor/MOR

µ Opioid Receptor/MOR mediates opioid analgesia as a heptahelical G protein-coupled receptor (GPCR) and suppresses cellular activity through predominantly Gᵢ/ₒ-coupled signaling^[1]^[2]. Mechanistically, MOR activation inhibits the adenylyl cyclase/cAMP pathway, activates inwardly rectifying potassium channels, and inhibits voltage-dependent calcium channels, linking receptor signaling to reduced pain transmission^[2]. In pain models, MOR signaling is regulated by receptor phosphorylation, β-arrestin2 recruitment, desensitization, internalization, and agonist-dependent endocytosis^[3]^[4]. In disease models, altered MOR-mediated G-protein activation appears in schizophrenia-relevant rat brain regions and HIV-1 Tat-exposed mouse forebrain regions^[5]^[6]. Compared with related isoforms, OPRM1 alternative splicing generates full-length 7TM, truncated 6TM, and single-transmembrane variants, and these isoforms show different trafficking, G-protein activation, β-arrestin2 recruitment, and biased signaling^[7]^[8]. The 6TM MOR1K isoform differs from MOR1 because morphine stimulation increases Ca²⁺ and nitric oxide release and couples to stimulatory Gαs, whereas MOR1 couples to inhibitory Gαᵢ/ₒ^[9]. For experimental applications, DAMGO, morphine, fentanyl, methadone, and receptor inhibitors support studies of MOR signaling, endocytosis, analgesia, tolerance, and disease-associated receptor function^[3]^[4]^[10].

References:

[1]. Pasternak G, et al. Mu opioid receptors in pain management. Acta Anaesthesiol Taiwan. 2011 Mar;49(1):21-5. [Content Brief]

[2]. Gris P, et al. Molecular assays for characterization of alternatively spliced isoforms of the u opioid receptor (MOR). Methods Mol Biol. 2010;617:421-35. [Content Brief]

[3]. Abdullah N, et al. TRPV1 and MOR working in tandem: implications for pain and opioids use. Neuropsychopharmacology. 2020 Jan;45(1):225-226. [Content Brief]

[4]. Campa VM, et al. Endocytosis as a biological response in receptor pharmacology: evaluation by fluorescence microscopy. PLoS One. 2015 Apr 7;10(4):e0122604. [Content Brief]

[5]. Szűcs E, et al. Mu-Opioid (MOP) receptor mediated G-protein signaling is impaired in specific brain regions in a rat model of schizophrenia. Neurosci Lett. 2016 Apr 21;619:29-33. [Content Brief]

[6]. Hahn YK, et al. Central HIV-1 Tat exposure elevates anxiety and fear conditioned responses of male mice concurrent with altered mu-opioid receptor-mediated G-protein activation and β-arrestin 2 activity in the forebrain. Neurobiol Dis. 2016 Aug;92(Pt B):124-36. [Content Brief]

[7]. Xu J, et al. Isolating and characterizing three alternatively spliced mu opioid receptor variants: mMOR-1A, mMOR-1O, and mMOR-1P. Synapse. 2014 Apr;68(4):144-52. [Content Brief]

[8]. Narayan A, et al. Mu Opioids Induce Biased Signaling at the Full-Length Seven Transmembrane C-Terminal Splice Variants of the mu Opioid Receptor Gene, Oprm1. Cell Mol Neurobiol. 2021 Jul;41(5):1059-1074. [Content Brief]

[9]. Gris P, et al. A novel alternatively spliced isoform of the mu-opioid receptor: functional antagonism. Mol Pain. 2010 Jun 2;6:33. [Content Brief]

[10]. Bouchet CA, et al. Mice Expressing Regulators of G protein Signaling-insensitive Gαo Define Roles of μ Opioid Receptor Gαo and Gαi Subunit Coupling in Inhibition of Presynaptic GABA Release. Mol Pharmacol. 2021 Sep;100(3):217-223. [Content Brief]

Productos relacionados con μ Opioid Receptor/MOR (128):

By Type:	Pan (25) Selective (22)
By Effects:	Inhibitors (5) Agonists (65) Antagonists (36) Activators (3) Modulators (9) Ligands (2)

Cat. No.	Nombre del producto	Efecto	Pureza

HY-P0244A

Dermorphin TFA	Agonist
Dermorphin TFA is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain.

HY-P3870

DALDA	Agonist
DALDA is a potent and highly selective μ-opioid receptor agonist with a K_i of 1.69 nM. DALDA shows antinociceptive and respiratory effects.

HY-162552

KOR/DOR agonist 1	Agonist
KOR/DOR agonist 2 is a KOR and DOR opioid receptors agonist with K_i values of 0.14 nM, and 0.93 nM, respectively. KOR/DOR agonist 2 shows significant antinociceptive effects. KOR/DOR agonist 2 penetrates the blood-brain barrier.

HY-P10177

Acetalin-3	Antagonist
Acetalin-3 (Ac-RFMWMT-NH2), a hexapeptide, is a μ opioid receptor antagonist with high affinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors.

HY-145369

DS34942424	Modulator
DS34942424 is an orally potent analgesic without mu opioid receptor agonist activity.

HY-106601

Picenadol
Picenadol (LY-150720) is an opioid mixed agonist-antagonist analgesic. Picenadol is an external racemic mixture, where its d-isomer (LY136596) is a potent μ-opioid receptor agonist, and the l-isomer (LY136595) is a weak μ-receptor competitive antagonist, which can inhibit the agonist effect and reduce the risk of dependence. Picenadol has anticholinergic activity.

HY-105525

Sameridine	Agonist
Sameridine (NIH-10908 free base) is a weak partial agonist of the μ-opioid receptor. Sameridine shows local anesthetic and analgesic properties. Sameridine has minimal respiratory depression at low doses, but can suppress ventilatory response at high doses. Sameridine can be used for the study of analgesic effect.

HY-172865

3,4-Methylenedioxy U-47700 hydrochloride	Agonist
3,4-Methylenedioxy U-47700 (3,4-MDO-U-47700) hydrochloride is a psychoactive substance and a complete agonist of μ-opioid receptor.

HY-185356

SR-14968	Agonist
SR-14968 is a full, allosteric and non-competitive MOR agonist, with an EC₅₀ of 88 nM for MOR in mouse brainstem. SR-14968 stabilizes MOR in a G protein signaling state that is resistant to washout but reversible by antagonists. SR-14968 induces respiratory depression in mice. SR-14968 can be used in pain-related research.

HY-P3044

Bilaid A1e	Agonist
Bilaid A1e (Compound 1e) is a tetrapeptide agonist of the µ-opioid receptor (K_i = 750 nM). Bilaid A1e can be isolated from an Australian estuarine isolate of Penicillium sp. Bilaid A1e can be used for pain research.

HY-118615

LY2048978	Antagonist
LY2048978 is a non-selective opioid receptor antagonist with K_i of 0.287, 0.471 and 1.05 nM for human mu, kappa and delta opioid receptors in vitro, respectively. LY2048978 can be used in the research of major depressive disorder and alcohol use disorder.

HY-144610

Mu opioid receptor antagonist 5	Antagonist
Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with an EC₅₀ value of 1.14 nM and a K_i value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD).

HY-W1121939

Perillyl acetate	Agonist
Perillyl acetate is a monoterpene found in in essential oils of plants and is synthesized from perillyl alcohol (HY-N7000). Perillyl acetate can activate the μ-opioid receptor and exert potent analgesic activity. Perillyl acetate can be used for the research of inflammation and neurological disease such as arthritis.

HY-185355

μ Opioid receptor agonist 4	Agonist
μ Opioid receptor agonist 4 (Compound 104) acts as an agonist of the μ-opioid receptor (MOP). μ Opioid receptor agonist 4 produces analgesic effects in mice, with a potency 2300-fold higher than that of Meperidine.

HY-175661

SRI-22136	Antagonist
SRI-22136 is a Delta Opioid Receptor (DOR) antagonist that can cross blood-brain barrier with a IC₅₀ of 0.42 nM. SRI-22136 does not have agonistic activity but antagonistic activity against DOR, MOR (IC₅₀ = 370 nM), KOR (IC₅₀ = 54 nM) and can avoid addiction/aversion effects. SRI-22136 can effectively inhibit the BACE1 activity induced by DADLE (a DOR agonist) (HY-105343) (IC₅₀ = 120 nM). SRI-22136 prevents completely Alzheimer’s-like pathology in mouse model. SRI-22136 can used for the study of Alzheimer’s disease.

HY-144608

Mu opioid receptor antagonist 3	Antagonist
Mu opioid receptor antagonist 3 (compound 26) is a potent and selective μ opioid receptor (MOR) antagonist with a K_i of 0.24 nM and an EC₅₀ of 0.54 nM. Mu opioid receptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 3 can be used for researching opioid use disorders (OUD).

HY-170310

AP-238	Agonist
AP-238 is a a new synthetic opioid (NSO), and acts as an agonist for μ-opioid receptor (MOR) with an EC₅₀ of 248 nM. AP-238 exhibits analgesic activity.

HY-W158948

6-Fluoro-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole	Modulator
6-Fluoro-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole is a ORL-1 receptor modulator. 6-Fluoro-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole regulates downstream pathways associated with nociception, cognition and physiological processes. 6-Fluoro-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole is used in the research of central nervous system diseases and pain-related disorders including anxiety, depression, Alzheimer's disease and attention deficit disorder.

HY-177218

M119
M119 (NSC 119910) is a selective Gβγ-subunit inhibitor. M119 selectively potentiates μ-opioid-dependent antinociception. M119 inhibits μ-receptor-dependent phospholipase (PLC) activation. M119 can enhance opioid analgesia and attenuate its acute tolerance and dependence in mice. M119 can be used for pain research.

HY-112692A

AT-121 hydrochloride	Agonist
AT-121 hydrochloride is a bifunctional nociception and mu opioid receptor agonist, with K_is of 3.67 and 16.49 nM, respectively. AT-121 hydrochloride is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects.

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