MR-2034
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| Other names | MR2034; Mr-2034; (–)-MR-2033; (–)-MR2033 |
| Drug class | κ-Opioid receptor agonist; Hallucinogen |
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| Formula | C19H27NO2 |
| Molar mass | 301.430 g·mol−1 |
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MR-2034, or Mr-2034, also known as (–)-MR-2033, is a selective κ-opioid receptor (KOR) agonist of the benzomorphan family.[1][2] Unlike other benzomorphan KOR agonists like cyclazocine and alazocine, MR-2034 does not also act on sigma receptors.[2] In addition to the KOR, it has affinity for the μ-opioid receptor (MOR), but does not activate this receptor.[2] The drug produces dose-dependent hallucinogenic and dysphoric effects in humans, as well as other effects such as dizziness, anxiety, and sedation.[3][2] These effects can be blocked by the non-selective opioid receptor antagonist naloxone.[2] The preceding findings led to the conclusion that the hallucinogenic and dysphoric effects of benzomorphans are mediated by the KOR rather than by sigma receptors.[2] MR-2034 was first described in the scientific literature by 1975[4][5] and its hallucinogenic effects in humans were described in 1986.[2]
See also
[edit]References
[edit]- ↑ Coupar JM, Quinn MJ (May 1988). "The effects of the selective kappa-opioid agonist MR 2034 on the guinea-pig ileum". The Journal of Pharmacy and Pharmacology. 40 (5): 378–380. doi:10.1111/j.2042-7158.1988.tb05274.x. PMID 2899640.
- 1 2 3 4 5 6 7 Pfeiffer A, Brantl V, Herz A, Emrich HM (August 1986). "Psychotomimesis mediated by kappa opiate receptors". Science. 233 (4765): 774–776. doi:10.1126/science.3016896. PMID 3016896.
- ↑ Farahbakhsh ZZ, Siciliano CA (January 2026). "Kappa opioid receptor control of motivated behavior revisited". Neuropsychopharmacology. 51 (2): 383–398. doi:10.1038/s41386-025-02226-9. PMC 12708679. PMID 41083597.
- ↑ Kosterlitz HW, Hughes J (July 1975). "Some thoughts on the significance of enkephalin, the endogenous ligand". Life Sciences. 17 (1): 91–96. doi:10.1016/0024-3205(75)90243-x. PMID 806763.
- ↑ Hutchinson M, Kosterlitz HW, Leslie FM, Waterfield AA (December 1975). "Assessment in the guinea-pig ileum and mouse vas deferens of benzomorphans which have strong antinociceptive activity but do not substitute for morphine in the dependent monkey". British Journal of Pharmacology. 55 (4): 541–546. doi:10.1111/j.1476-5381.1975.tb07430.x. PMC 1666732. PMID 2359.
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