Cericlamine

Last updated
Cericlamine
Cericlamine.svg
Clinical data
Other namesJO-1017
Routes of
administration
Oral [1]
ATC code
  • None
Pharmacokinetic data
Elimination half-life 8 hours [1]
Identifiers
  • 3-(3,4-Dichlorophenyl)-2-(dimethylamino)-2-methylpropan-1-ol
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
Formula C12H17Cl2NO
Molar mass 262.17 g·mol−1
3D model (JSmol)
  • CC(CC1=CC(=C(C=C1)Cl)Cl)(CO)N(C)C
  • InChI=1S/C12H17Cl2NO/c1-12(8-16,15(2)3)7-9-4-5-10(13)11(14)6-9/h4-6,16H,7-8H2,1-3H3
  • Key:FWYRGHMKHZXXQX-UHFFFAOYSA-N

Cericlamine (INN; developmental code JO-1017) is a potent and moderately selective serotonin reuptake inhibitor (SSRI) of the amphetamine family (specifically, a derivative of phentermine, and closely related to chlorphentermine, a highly selective serotonin releasing agent) that was investigated as an antidepressant for the treatment of depression, anxiety disorders, and anorexia nervosa by Jouveinal but did not complete development and was never marketed. [1] [2] [3] [4] It reached phase III clinical trials in 1996 before development was discontinued in 1999. [5]

According to Czech scientists, cericlamine is claimed to be part of a highly advanced “fifth generation” of antidepressants as was venlafaxine. [6]

The daily dosage was reported to be 300mg. [1]

See also

Related Research Articles

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References

  1. 1 2 3 4 Darcourt G, Tessera M, Lesaunier R, Engrand P, Scherrer B, Dreyfus J, Bogaievsky Y (1992). "A Multicentre Double-Blind, Placebo-Controlled Dose-Finding Study with Cericlamine in Major Depression". Clinical Neuropharmacology. 15: 176B. doi:10.1097/00002826-199202001-00339. ISSN   0362-5664. S2CID   57983762.
  2. Crow S, Brown E (March 2003). "Investigational drugs for eating disorders". Expert Opinion on Investigational Drugs. 12 (3): 491–9. doi:10.1517/13543784.12.3.491. PMID   12605570. S2CID   25463729.
  3. Patel RM (3 January 2000). Stereoselective Biocatalysis. CRC Press. pp. 48–. ISBN   978-0-8247-8282-5.
  4. Tang LC, Tang SJ (6 December 2012). Neurochemistry in Clinical Application. Springer Science & Business Media. pp. 81–. ISBN   978-1-4615-1857-0.
  5. "Cericlamine". AdisInsight. Springer Nature Switzerland AG. Retrieved 13 January 2016.
  6. Svestka, J. (1994). "Antidepressives of the 3rd, 4th and 5th generation". Ceskoslovenska Psychiatrie. 90 (1): 3–19. PMID   8174184.