Ciclazindol

Ciclazindol (WY-23409) is an antidepressant and anorectic drug of the tetracyclic chemical class that was developed in the mid to late 1970s, but was never marketed.[2][3] It acts as a norepinephrine reuptake inhibitor, and to a lesser extent as a dopamine reuptake inhibitor.[2][4] Ciclazindol has no effects on the SERT, 5-HT receptors, mACh receptors, or α-adrenergic receptors, and has only weak affinity for the H1 receptor.[4][5][6] As suggested by its local anesthetic properties,[5] ciclazindol may also inhibit sodium channels. It is known to block potassium channels as well.[7][8]

Ciclazindol
Clinical data
Routes of
administration		Oral
ATC code
  • none
Pharmacokinetic data
MetabolismRenal[1]
Elimination half-life~32 hours[1]
ExcretionUrine, feces[1]
Identifiers
IUPAC name
  • 10-(3-chlorophenyl)-3,4-dihydro-2H-pyrimido[1,2-a]indol-10-ol
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC17H15ClN2O
Molar mass298.77 g·mol−1
3D model (JSmol)
SMILES
  • Clc1cccc(c1)C3(O)c4c(N2\C3=N/CCC2)cccc4

See also

References
  1. Swaisland AJ, Franklin RA, Southgate PJ, Coleman AJ (February 1977). "The pharmacokinetics of ciclazindol (Wy 23409) in human volunteers". British Journal of Clinical Pharmacology. 4 (1): 61–5. doi:10.1111/j.1365-2125.1977.tb00668.x. PMC 1428987. PMID 843425.
  2. Ghose K, Rama Rao VA, Bailey J, Coppen A (April 1978). "Antidepressant activity and pharmacological interactions of ciclazindol". Psychopharmacology. 57 (1): 109–14. doi:10.1007/BF00426966. PMID 96461. S2CID 12961802.
  3. Levine S (1979). "A controlled comparative trial of a new antidepressant, ciclazindol". The Journal of International Medical Research. 7 (1): 1–6. doi:10.1177/030006057900700101. PMID 369921. S2CID 28112402.
  4. Oh VM, Ehsanullah RS, Leighton M, Kirby MJ (January 1979). "Influence of ciclazindol on monoamine uptake and CNS function in normal subjects". Psychopharmacology. 60 (2): 177–81. doi:10.1007/BF00432290. PMID 106428. S2CID 24199961.
  5. Waterfall JF, Smith MA, Gaston WH, Maher J, Warburton G (July 1979). "Cardiovascular and autonomic actions of ciclazindol and tricyclic antidepressants". Archives Internationales de Pharmacodynamie et de Thérapie. 240 (1): 116–36. PMID 507990.
  6. Gardner CR, Wilford AE (January 1980). "The effects of mianserine, amitriptyline, ciclazindol and viloxazine on presynaptic alpha-receptors in isolated rat atria [proceedings]". British Journal of Pharmacology. 68 (1): 184P–185P. doi:10.1111/j.1476-5381.1980.tb10705.x. PMC 2044122. PMID 6244029.
  7. Noack T, Edwards G, Deitmer P, et al. (May 1992). "The involvement of potassium channels in the action of ciclazindol in rat portal vein". British Journal of Pharmacology. 106 (1): 17–24. doi:10.1111/j.1476-5381.1992.tb14286.x. PMC 1907450. PMID 1504725.
  8. Lee K, Khan RN, Rowe IC, et al. (April 1996). "Ciclazindol inhibits ATP-sensitive K+ channels and stimulates insulin secretion in CR1-G1 insulin-secreting cells". Molecular Pharmacology. 49 (4): 715–20. PMID 8609901.


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