Target intelligence / Profile preview

Mu-type opioid receptor mRNA (OPRM1 mRNA) (OPRM1 mRNA)

Target
OPRM1 mRNA
Molecular classification
Other (mRNA), Nucleic acid
01

Overview

The OPRM1 mRNA is the primary transcript of the OPRM1 gene, which encodes the Mu-type opioid receptor (MOR), a G protein-coupled receptor essential for the analgesic effects of both endogenous and exogenous opioids [1, 2]. This mRNA is notable for its extensive alternative splicing, which generates numerous isoforms that vary in their C-terminal sequences, influencing receptor trafficking, signaling efficiency, and the pharmacological profile of opioid ligands [3, 5]. While the MOR protein is the direct target of drugs like morphine and fentanyl, the OPRM1 mRNA is a target for experimental therapeutic strategies, including antisense oligonucleotides (ASOs) and RNA interference (RNAi), designed to modulate receptor expression or selectively target specific splice variants [4, 5]. Such approaches aim to mitigate opioid-related side effects, such as respiratory depression and physical dependence, by fine-tuning the opioid system at the post-transcriptional level [3, 5]. Additionally, variations in OPRM1 mRNA expression and the presence of single nucleotide polymorphisms (SNPs) like A118G are significant biomarkers for individual differences in pain sensitivity and susceptibility to opioid use disorder [2, 6].

Other names
MOR-1 mRNAOpioid receptor mu 1 mRNAOPRM1 transcriptMu opioid receptor mRNA
02

Mechanism of action

Antisense-mediated degradation of mRNA, inhibition of translation, and modulation of alternative splicing via splice-switching oligonucleotides [4, 5].

03

Biological functions

Signal transductionOther (Translation)Other (Alternative splicing)
04

Disease associations

Other (Opioid use disorder)Other (Chronic pain)Other (Drug addiction)
05

Safety considerations

Off-target RNA bindingCNS delivery challengesPotential for long-term alteration of pain sensitivityImmunogenicity of RNA-based therapeutics
06

Interacting drugs

Antisense oligonucleotides (experimental)

3 more in the full profile.

07

Biomarkers

OPRM1 mRNA expression levelsOPRM1 splice variant ratios (e.g., MOR-1 vs MOR-1K)A118G polymorphism (rs1799971)

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