Chemistry:Noribogainalog

From HandWiki

Noribogainalog (nor-IBG), also known as 9-hydroxyibogaminalog or as GATC-021, is a drug of the ibogalog family related to noribogaine.[1][2][3] It is a simplified analogue of noribogaine.[1][2]

Pharmacology

Pharmacodynamics

Noribogainalog acts as a potent serotonin 5-HT2A receptor partial agonist (EC50 ≈ 90 nM; Emax = 35–45%).[2][3] It is also a partial agonist of the serotonin 5-HT6 receptor (Emax = 29%), whereas it is not an agonist of the serotonin 5-HT2B and 5-HT7 receptors.[3] The drug additionally has activity as a dopamine transporter (DAT) chaperone.[4]

Noribogainalog does not affect locomotor activity, does not produce the head-twitch response, and does not affect various other physiological and behavioral measures.[2] However, it does produce analgesic effects that can be diminished by the serotonin 5-HT2A receptor antagonist ketanserin.[2] In addition, a subsequent study found that the highest assessed dose produced significant hypolocomotion and that the drug also reduced fentanyl self-administration.[3]

Pharmacokinetics

Noribogainalog shows relatively low expected blood–brain barrier permeability.[2]

Chemistry

Synthesis

The chemical synthesis of noribogainalog has been described.[3]

Analogues

Analogues of noribogainalog include catharanthalog, ibogainalog, ibogaminalog, PNU-22394, tabernanthalog, 4-allyl-6-oxa-noribogainalog, and noribogaine, among others.

History

Noribogainalog was first described in the scientific literature by David E. Olson and colleagues by 2021.[1]

See also

  • Ibogalog

References

  1. ↑ 1.0 1.1 1.2 "A non-hallucinogenic psychedelic analogue with therapeutic potential". Nature 589 (7842): 474–479. January 2021. doi:10.1038/s41586-020-3008-z. PMID 33299186. Bibcode: 2021Natur.589..474C. 
  2. ↑ 2.0 2.1 2.2 2.3 2.4 2.5 "Ibogalogs decrease neuropathic pain in mice through a mechanism involving crosstalk between 5-HT2A and mGlu2 receptors". Biomedicine & Pharmacotherapy 184. March 2025. doi:10.1016/j.biopha.2025.117887. PMID 39938347. 
  3. ↑ 3.0 3.1 3.2 3.3 3.4 "AI-derived therapeutic development of a serotonin receptor-targeting drug for the treatment of opioid use disorder". Proc Natl Acad Sci U S A 123 (15). April 2026. doi:10.1073/pnas.2516807123. PMID 41941629. 
  4. ↑ "Structure-Activity Relationships of Dopamine Transporter Pharmacological Chaperones". Frontiers in Cellular Neuroscience 16. 2022. doi:10.3389/fncel.2022.832536. PMID 35614973. 



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