GT-2203
Pharmaceutical compound
From Wikipedia, the free encyclopedia
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]
administrationUnspecified[1]
- None
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| Other names | VUF-5296; (1R,2R)-Cyclopropylhistamine; (1R,2R)-trans-2-(1H-imidazol-4-yl)cyclopropylamine |
| Routes of administration | Unspecified[1] |
| Drug class | Histamine H3 receptor agonist |
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| Formula | C6H9N3 |
| Molar mass | 123.159 g·mol−1 |
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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
- BP 2.94
- Cipralisant (GT-2331)
- Pitolisant
- SCH-50971