Chemistry:Ciclazindol

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Short description: Chemical compound
Ciclazindol
Ciclazindol structure.svg
Clinical data
Routes of
administration		Oral
ATC code
  • none
Pharmacokinetic data
MetabolismRenal[1]
Elimination half-life~32 hours[1]
ExcretionUrine, feces[1]
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC17H15ClN2O
Molar mass298.77 g·mol−1
3D model (JSmol)

Ciclazindol (WY-23409) is an antidepressant and anorectic[2] drug of the tetracyclic[citation needed] chemical class that was developed in the mid to late 1970s, but was never marketed.[3][4] It acts as a norepinephrine reuptake inhibitor, and to a lesser extent as a dopamine reuptake inhibitor.[3][5] 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.[5][6][7] As suggested by its local anesthetic properties,[6] ciclazindol may also inhibit sodium channels. It is known to block potassium channels as well.[8][9]

The dosage in human volunteers is stated to be 25mg daily.[1] However, doses of up to 200mg have also been reported.[2] This is surprising since the dosage of mazindol is only 2-4mg per day.

Ciclazindol is reported to have an IC50 of 1.3nM for the dopamine transporter (cmp 23).[10]

See also

References

  1. ↑ 1.0 1.1 1.2 1.3 "The pharmacokinetics of ciclazindol (Wy 23409) in human volunteers". British Journal of Clinical Pharmacology 4 (1): 61–65. February 1977. doi:10.1111/j.1365-2125.1977.tb00668.x. PMID 843425. 
  2. ↑ 2.0 2.1 "Ciclazindol: an oral agent with weight reducing properties and hypoglycaemic activity". European Journal of Clinical Pharmacology 25 (1): 41–5. 1983. doi:10.1007/BF00544012. PMID 6352281. 
  3. ↑ 3.0 3.1 "Antidepressant activity and pharmacological interactions of ciclazindol". Psychopharmacology 57 (1): 109–114. April 1978. doi:10.1007/BF00426966. PMID 96461. 
  4. ↑ "A controlled comparative trial of a new antidepressant, ciclazindol". The Journal of International Medical Research 7 (1): 1–6. 1979. doi:10.1177/030006057900700101. PMID 369921. 
  5. ↑ 5.0 5.1 "Influence of ciclazindol on monoamine uptake and CNS function in normal subjects". Psychopharmacology 60 (2): 177–181. January 1979. doi:10.1007/BF00432290. PMID 106428. 
  6. ↑ 6.0 6.1 "Cardiovascular and autonomic actions of ciclazindol and tricyclic antidepressants". Archives Internationales de Pharmacodynamie et de Therapie 240 (1): 116–136. July 1979. PMID 507990. 
  7. ↑ "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. January 1980. doi:10.1111/j.1476-5381.1980.tb10705.x. PMID 6244029. 
  8. ↑ "The involvement of potassium channels in the action of ciclazindol in rat portal vein". British Journal of Pharmacology 106 (1): 17–24. May 1992. doi:10.1111/j.1476-5381.1992.tb14286.x. PMID 1504725. 
  9. ↑ "Ciclazindol inhibits ATP-sensitive K+ channels and stimulates insulin secretion in CR1-G1 insulin-secreting cells". Molecular Pharmacology 49 (4): 715–720. April 1996. PMID 8609901. http://molpharm.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8609901. 
  10. ↑ "Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter". Journal of Medicinal Chemistry 39 (25): 4935–4941. December 1996. doi:10.1021/jm960288w. PMID 8960553. 



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