m-opioid

CID 16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast.

AR-M 1000390 hydrochloride (ARM-390 HCl) , also known as ARM-390, is a low-internalizing nonpeptidic δ-selective opioid receptor agonist; derivative of SNC 80. Does not trigger acute desensitization of the analgesic response; reduces CFA-induced hyperalgesia. Brain penetrant following systemic administration.

VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR ( IC 50 =36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA) [1] [2] .

Mitraciliatine, an alkaloid discovered in M. speciosa (Kratom in Thai), acts as a partial agonist for the μ-opioid receptor (MOR) and an agonist for the κ-opioid receptor (KOR), demonstrating selectivity for these receptors over the δ-opioid receptor (DOR) with EC50 values of 228, 218, and >1,000 nM respectively in mouse receptors through a GTPγS binding assay. When administered intracerebroventricularly (i.c.v.) at 100 nmol/animal, mitraciliatine increases latency to withdrawal in the warm water tail withdrawal assay in mice, an effect reversable by MOR knockout but unaffected by KOR knockout, distinguishing it from morphine by not causing hyperlocomotion or respiratory depression.

AR-M 1000390 is an effective selective δ-opioid receptor agonist with an EC50 of 7.2±0.9 nM.

Dermorphin Analog, an analog of Dermorphin, is a natural heptapeptide μ-opioid receptor agonist found in amphibian skin. The dermorphin-derived peptide [Dmt1] Dermorphin Analog labels μ-opioid receptors with high affinity and selectivity in receptor binding assays.