Chemistry:GT-2203

From HandWiki

GT-2203, also known as VUF-5296, (1R,2R)-cyclopropylhistamine, or (1R,2R)-trans-2-(1H-imidazol-4-yl)cyclopropylamine, is a histamine H3 receptor agonist which was under development for the treatment of insomnia and anxiety disorders but was never marketed.[1][2][3] Its route of administration was unspecified.[1]

Pharmacology

The drug is a synthetic derivative of the neurotransmitter histamine.[3] The other enantiomer, (1S,2S)-cyclopropylhistamine (VUF-5297), is about 10-fold more potent than GT-2203 as a histamine H3 receptor agonist.[3] Both enantiomers are partial agonists of the receptor and both enantiomers show additional weak activity at the histamine H1 and H2 receptors.[3]

History

GT-2203 was under development by Gliatech.[1][2] It reached the preclinical research stage of development for insomnia and anxiety disorders prior to the discontinuation of its development in 2004.[1][2] The drug was first described in the scientific literature by 1997.[4] Aside from immethridine (BP-1-5375), GT-2203 is the only other selective histamine H3 receptor agonist to have been developed for potential pharmaceutical use.[1][5][6]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 "GT 2203". 16 September 2004. https://adisinsight.springer.com/drugs/800008938. 
  2. ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on GT-2203 with Synapse". 13 September 2025. https://synapse.patsnap.com/drug/385edd182ef14904852e55655174da2b. 
  3. ↑ 3.0 3.1 3.2 3.3 "Characterization of the binding site of the histamine H3 receptor. 1. Various approaches to the synthesis of 2-(1H-imidazol-4-yl)cyclopropylamine and histaminergic activity of (1R,2R)- and (1S,2S)-2-(1H-imidazol-4-yl)-cyclopropylamine". Journal of Medicinal Chemistry 42 (7): 1115–1122. April 1999. doi:10.1021/jm9810912. PMID 10197956. https://research.vu.nl/en/publications/3df1f0bf-d297-4070-8fd2-2bf527e76649. 
  4. ↑ "Diastereoselective synthesis of trans-2-(1-triphenylmethyl-1H-imidazol-4-yl)cyclopropanecarboxylic acids: key intermediates for the preparation of potent and chiral histamine H3 receptor agents". Bioorganic & Medicinal Chemistry Letters 7 (23): 3017–3022. 1997. doi:10.1016/S0960-894X(97)10137-8. https://linkinghub.elsevier.com/retrieve/pii/S0960894X97101378. Retrieved 27 September 2025. 
  5. ↑ "Immethridine". 16 July 2016. https://adisinsight.springer.com/drugs/800039144. 
  6. ↑ "Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist". Journal of Medicinal Chemistry 47 (10): 2414–2417. May 2004. doi:10.1021/jm049932u. PMID 15115383. 



Retrieved from "https://handwiki.org/wiki/index.php?title=Chemistry:GT-2203&oldid=4038433"