Methylsamidorphan chloride

A detailed overview of Methylsamidorphan chloride

{{Drugbox | Verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = (2S)-2-[[4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]methyl]-1-methylpyrrolidine hydrochloride | image = Methylsamidorphan_structure.png | width = 200 | CAS_number = 123456-78-9 | PubChem = 12345678 | ChemSpiderID = 123456 | UNII = 123456789A | KEGG = D12345 | ChEMBL = 1234567 | C=21 | H=30 | N=2 | O=1 | Cl=1 | molecular_weight = 364.93 g/mol }}

Methylsamidorphan chloride is a chemical compound that acts as a potent opioid receptor modulator. It is primarily studied for its potential use in combination therapies for the treatment of opioid use disorder and major depressive disorder.

Pharmacology

Methylsamidorphan chloride is known to function as a mixed opioid receptor modulator. It exhibits partial agonist activity at the mu-opioid receptor and antagonist activity at the kappa-opioid receptor. This dual action is thought to contribute to its therapeutic effects, particularly in reducing the risk of opioid dependence and mitigating depressive symptoms.

Mechanism of Action

The compound's mechanism of action involves modulation of the opioid receptor system. By acting as a partial agonist at the mu-opioid receptor, methylsamidorphan chloride can provide analgesic effects while minimizing the risk of addiction. Its antagonist activity at the kappa-opioid receptor is associated with antidepressant effects, as kappa-opioid receptor activation is often linked to dysphoria and depressive symptoms.

Clinical Applications

Methylsamidorphan chloride is being investigated for its potential use in combination with other medications, such as buprenorphine and naloxone, to enhance treatment outcomes for patients with opioid use disorder. Additionally, its antidepressant properties are being explored in clinical trials for patients with treatment-resistant depression.

Safety and Efficacy

Clinical trials have demonstrated that methylsamidorphan chloride is generally well-tolerated, with a safety profile similar to other opioid receptor modulators. Common side effects include nausea, headache, and dizziness. Its efficacy in reducing opioid cravings and improving mood symptoms has been promising, though further research is needed to fully establish its therapeutic potential.

Research and Development

Ongoing research is focused on optimizing the dosing regimen of methylsamidorphan chloride and evaluating its long-term effects. Studies are also exploring its potential use in other psychiatric and neurological disorders, given its unique pharmacological profile.

Also see

• Opioid receptor
• Opioid use disorder
• Major depressive disorder
• Buprenorphine
• Naloxone