Gevotroline (WY-47,384) is an atypical antipsychotic with a tricyclic structure which was under development for the treatment of schizophrenia by Wyeth-Ayerst.[1][2][3] It acts as a balanced, modest affinity D2 and 5-HT2 receptor antagonist and also possesses high affinity for the sigma receptor.[2][4][5][6] It was well tolerated and showed efficacy in phase II clinical trials but was never marketed.[2][3]

Gevotroline
Clinical data
Routes of
administration
Oral
ATC code
  • None
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • 8-fluoro-2-(3-pyridin-3-ylpropyl)-1,3,4,5-tetrahydropyrido[4,3-b]indole
CAS Number
PubChem CID
ChemSpider
UNII
ChEBI
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H20FN3
Molar mass309.388 g·mol−1
3D model (JSmol)
  • Fc2cc1c3c([nH]c1cc2)CCN(C3)CCCc4cccnc4

See also

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References

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  1. ^ Triggle DJ (1996). Dictionary of Pharmacological Agents. Boca Raton: Chapman & Hall/CRC. ISBN 0-412-46630-9.
  2. ^ a b c Abou-Gharbia M, Moyer JA (1990). Bristol JA (ed.). "Novel Antipyschotic Agents". Annual Reports in Medicinal Chemistry. 25. Boston: Academic Press: 1–10. doi:10.1016/S0065-7743(08)61577-8. ISBN 0-12-040525-3.
  3. ^ a b Jackson DM, Mohell N (1996). "A Review of the Pharmacology of New Antipsychotic Drugs". In Stone TW (ed.). CNS neurotransmitters and neuromodulators: dopamine. Boca Raton: CRC Press. ISBN 0-8493-7632-7.
  4. ^ Snyder SH, Largent BL (1989). "Receptor mechanisms in antipsychotic drug action: focus on sigma receptors". The Journal of Neuropsychiatry and Clinical Neurosciences. 1 (1): 7–15. doi:10.1176/jnp.1.1.7. PMID 2577720.
  5. ^ Matheson GK, Guthrie D, Bauer C, Knowles A, White G, Ruston C (January 1991). "Sigma receptor ligands alter concentrations of corticosterone in plasma in the rat". Neuropharmacology. 30 (1): 79–87. doi:10.1016/0028-3908(91)90046-E. PMID 1675451. S2CID 29702968.
  6. ^ Gudelsky GA, Nash JF (February 1992). "Neuroendocrinological and neurochemical effects of sigma ligands". Neuropharmacology. 31 (2): 157–162. doi:10.1016/0028-3908(92)90026-L. PMID 1348112. S2CID 36585024.