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. It acts as a norepinephrine reuptake inhibitor, and to a lesser extent as a dopamine reuptake inhibitor. 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. As suggested by its local anesthetic properties, ciclazindol may also inhibit sodium channels. It is known to block potassium channels as well.

Ciclazindol
Clinical data
Routes of
administration		Oral
ATC code
  • none
Pharmacokinetic data
MetabolismRenal
Elimination half-life~32 hours
ExcretionUrine, feces
Identifiers
  • 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)
  • Clc1cccc(c1)C3(O)c4c(N2\C3=N/CCC2)cccc4

The dosage in human volunteers is stated to be 25mg daily. However, doses of up to 200mg have also been reported. 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).

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