Gavestinel
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| Systematic (IUPAC) name | |
| 3-[(E)-3-anilino-3-oxoprop-1-enyl]-4,6-dichloro-1H-indole-2-carboxylic acid | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 153436-22-7  |
| ATC code | None |
| PubChem | CID 6450546 |
| ChemSpider | 4953148  |
| UNII | 318X4QY113 |
| ChEMBL | CHEMBL419045 |
| Synonyms | GV-150,526A |
| Chemical data | |
| Formula | C18H12Cl2N2O3 |
| Mol. mass | 375.205 g/mol |
| SMILES | eMolecules & PubChem |
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Gavestinel (GV-150,526) is a drug which acts as an NMDA antagonist, binding selectively to the glycine site on the NMDA receptor complex, rather than the glutamate site many NMDA antagonists bind to.[1] It is neuroprotective in animal studies and has been researched for the treatment of stroke, progressing as far as Phase II clinical trials in humans before being dropped for lack of efficacy.[2][3][4][5] Gavestinel lacks phencyclidine-like behavioural effects in animals and is considered unlikely to possess any abuse potential in humans.[6]
[edit] References
- ^ Chopra B, Chazot PL, Stephenson FA. Characterization of the binding of two novel glycine site antagonists to cloned NMDA receptors: evidence for two pharmacological classes of antagonists. British Journal of Pharmacology. 2000 May;130(1):65-72. PMID 10780999
- ^ Di Fabio R, Capelli AM, Conti N, Cugola A, Donati D, Feriani A, Gastaldi P, Gaviraghi G, Hewkin CT, Micheli F, Missio A, Mugnaini M, Pecunioso A, Quaglia AM, Ratti E, Rossi L, Tedesco G, Trist DG, Reggiani A (March 1997). "Substituted indole-2-carboxylates as in vivo potent antagonists acting as the strychnine-insensitive glycine binding site". Journal of Medicinal Chemistry 40 (6): 841–50. doi:10.1021/jm960644a. PMID 9083472.
- ^ Bordi F, Pietra C, Ziviani L, Reggiani A (June 1997). "The glycine antagonist GV150526 protects somatosensory evoked potentials and reduces the infarct area in the MCAo model of focal ischemia in the rat". Experimental Neurology 145 (2 Pt 1): 425–33. doi:10.1006/exnr.1997.6442. PMID 9217078.
- ^ Lees KR, Lavelle JF, Cunha L, Diener HC, Sanders EA, Tack P, Wester P. Glycine antagonist (GV150526) in acute stroke: a multicentre, double-blind placebo-controlled phase II trial. Cerebrovascular Diseases. 2001;11(1):20-9. PMID 11173790
- ^ Haley EC, Thompson JL, Levin B, Davis S, Lees KR, Pittman JG, DeRosa JT, Ordronneau P, Brown DL, Sacco RL (May 2005). "Gavestinel does not improve outcome after acute intracerebral hemorrhage: an analysis from the GAIN International and GAIN Americas studies". Stroke; a Journal of Cerebral Circulation 36 (5): 1006–10. doi:10.1161/01.STR.0000163053.77982.8d. PMID 15831831.
- ^ Beardsley PM, Ratti E, Balster RL, Willetts J, Trist D (November 2002). "The selective glycine antagonist gavestinel lacks phencyclidine-like behavioral effects". Behavioural Pharmacology 13 (7): 583–92. PMID 12409996.
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