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]

μ Opioid Receptor/MOR Verwandte Produkte (128):

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

Art. -Nr.	Produktname	Wirkung	Reinheit

HY-W414109

ID110460002	Agonist
ID110460002 possesses both full agonist activity at the μ-opioid receptor (OPRM) and agonist activity at the δ-opioid receptor (OPRD). ID110460002 acts as a potent agonist for the G protein pathways of both receptors, but exhibits only very weak partial agonist activity towards the β-arrestin-2 pathway. The agonistic potency of ID110460002 at OPRM has extremely high intrinsic activity and is unaffected by reduced receptor expression levels, while its potency at OPRD depends on receptor expression levels. ID110460002 displays tissue- or organ-dependent properties, and serves as a critical compound for investigating pain mechanisms and analgesia.

HY-A0118AS

Naloxegol-d₅ oxalate	Antagonist
Naloxegol-d₅ (oxalate) is deuterium labeled Naloxegol (oxalate). Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.

HY-170437

MOR modulator-1	Modulator
MOR modulator-1 (compound 6) is a potent and selective μ opioid receptor (MOR) modulator. MOR modulator-1 exhibits improved opioid receptor selectivity, enhanced in vivo antagonistic effect, and overall fewer withdrawal symptoms compared to NAT (6α-configuration). MOR modulator-1 links with carboxamido linker μ, δ, γ with K_is of 0.25, 41.1, 1.30 nM, respectively_[1]

HY-181956

MPAM-15	Modulator
MPAM-15 is a blood-brain barrier-penetrant pan-orthosteric allosteric modulator (PAM) of opioid receptors, with ≥16-fold selectivity for μOR over δOR and κOR. MPAM-15 acts as an anti-nociceptive potentiator and analgesic, and its activity is observed in mouse models via both intracerebroventricular and intraperitoneal administration. MPAM-15 is applicable for pain-related research.

HY-171758

BU72	Agonist
BU72 is a highly potent and long-acting agonist of μ and κ opioid receptors, and also has a partial agonist effect on δ opioid receptors (EC₅₀ values are 0.054, 0.033, and 0.58 nM, respectively). BU72 has a strong and long-lasting analgesic effect, which is mainly mediated by μ opioid receptors. BU72 has a long-lasting activity and can partially reverse the analgesic effect of morphine. BU72 can be used in the study of opioid dependence.

HY-P10175

Acetalin-1	Antagonist
Acetalin-1 (Ac-RFMWMK-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-P1329

CTOP	Agonist
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity.

HY-16765

Axelopran	Antagonist
Axelopran (TD-1211) is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guinea pig κ receptor, respectively.

HY-B0380S2

Trimebutine-d₃ hydrochloride	Agonist
Trimebutine-d₃ hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

HY-107121

Ondelopran	Antagonist
Ondelopran (LY 2196044) is a non-selective opioid receptor antagonist. Ondelopran inhibits the release of dopamine in the nucleus accumbens induced by alcohol, reduces the rewarding effect of alcohol consumption, and lowers the craving. Ondelopran can be used for alcohol use disorder (AUD).

HY-173030

Opioid receptor agonist 1	Agonist
Opioid receptor agonist 1 (Compound 2638-28) is the orally active agonist for opioid receptor that exhibits good affinity to MOR, DOR and KOR with K_i of 5, 24 and 212 nM, respectively. Opioid receptor agonist 1 exhibits analgesic activity in mouse warm water tail flick models and acetic acid writhing models.

HY-155706

MOR agonist-2	Agonist
MOR agonist-2 (compound 46) is a antagonist of D3R and agonist of MOR (K_i: 7.26 nM and 564 nM, respectively). MOR agonist-2 has the potential to produce analgesic effects through MOR partial agonism. MOR agonist-2 reduces opioid-misuse liability via D3R antagonism.

HY-P1253

α-Endorphin (human)	Modulator
α-Endorphin (human) is a neuropeptide, that acts on the central nervous system (CNS) and peripheral nervous system (PNS). α-Endorphin (human) binds μ-opioid receptor, and exhibits analgesic efficacy. α-Endorphin (human) regulates sexual behaviors and pleasure felling.

HY-W399025

ID110460001	Agonist
ID110460001 is a full agonist of μ-opioid receptor and an agonist of δ-opioid receptor. ID110460001 exhibits high intrinsic efficacy for G protein pathway activation of μ-opioid receptor, and this property is not affected by the reduction in receptor quantity. ID110460001 acts only as a very weak partial agonist in the β-arrestin-2 pathway of both receptors, and binds to μ-opioid receptor via a specific mode. The efficacy of ID110460001 in the G protein pathway of δ-opioid receptor is sensitive to changes in receptor quantity. ID110460001 can be used in pain-related research.

HY-P1577

Dermorphin Analog	Agonist
Dermorphin Analog is an analog of Dermorphin. Dermorphin is a natural heptapeptide μ-opioid receptor agonist found in amphibian skin.

HY-B0380S1

Trimebutine-d₅ fumarate	Agonist
Trimebutine-d₅ fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

HY-179705

MOR agonist-5	Agonist
MOR agonist-5 is a selective and potent mu-opioid receptor (MOR) agonist with an EC₅₀ of 0.25 nM. MOR agonist-5 shows an EC₅₀ of 10 nM for DOR and >10000 nM for KOR and NOR. MOR agonist-5 exerts significant antinociceptive activity. MOR agonist-5 can be used for the research of pain.

HY-182453

RM1490	Modulator
RM1490 (Compound 251) acts as an inhibitor of μ-opioid receptor (MOR) (IC₅₀ ≤ 300 nM), an activator of δ-opioid receptor (DOR) (EC₅₀ > 3000 nM), and an inhibitor of κ-opioid receptor (KOR) (IC₅₀ ≤ 300 nM). RM1490 is applicable to the research of neuropsychiatric disorders.

HY-175486

KOR agonist 6	Agonist
KOR agonist 6 is a KOR agonist (K_i = 0.25 pM). KOR agonist 6 shows agonistic activity at MOR and DOR in CHO cells and inhibits Forskolin (HY-15371)-stimulated cAMP accumulation. KOR agonist 6 stimulates KOR-mediated [³⁵S]GTPγS binding and inhibits cAMP accumulation in KOR-expressing HEK293 cells with potent agonistic activity, while showing lower β-arrestin recruitment potency. KOR agonist 6 demonstrates anti-nociceptive efficacy in mice. KOR agonist 6 can be used for the study of analgesics with reduced central nervous system (CNS) side effects.

HY-B0380AR

Trimebutine maleate (Standard)	Agonist
Trimebutine maleate (Standard) is the analytical standard of Trimebutine maleate (HY-B0380A). This product is intended for research and analytical applications. Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca²⁺ channels and large-conductance calcium-activated potassium channels (BK_Ca channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).

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