Chemistry:MR-2034

From HandWiki

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]

References

  1. ↑ "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. May 1988. doi:10.1111/j.2042-7158.1988.tb05274.x. PMID 2899640. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 2.5 2.6 "Psychotomimesis mediated by kappa opiate receptors". Science 233 (4765): 774–776. August 1986. doi:10.1126/science.3016896. PMID 3016896. 
  3. ↑ "Kappa opioid receptor control of motivated behavior revisited". Neuropsychopharmacology 51 (2): 383–398. January 2026. doi:10.1038/s41386-025-02226-9. PMID 41083597. 
  4. ↑ "Some thoughts on the significance of enkephalin, the endogenous ligand". Life Sciences 17 (1): 91–96. July 1975. doi:10.1016/0024-3205(75)90243-x. PMID 806763. 
  5. ↑ "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. December 1975. doi:10.1111/j.1476-5381.1975.tb07430.x. PMID 2359. 



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