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Ciclazindol

Chemical compound

Chemical compound

| elimination_half-life = ~32 hours

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.

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

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

References

References

  1. (February 1977). "The pharmacokinetics of ciclazindol (Wy 23409) in human volunteers". British Journal of Clinical Pharmacology.
  2. (1983). "Ciclazindol: an oral agent with weight reducing properties and hypoglycaemic activity". European Journal of Clinical Pharmacology.
  3. (April 1978). "Antidepressant activity and pharmacological interactions of ciclazindol". Psychopharmacology.
  4. (1979). "A controlled comparative trial of a new antidepressant, ciclazindol". The Journal of International Medical Research.
  5. (January 1979). "Influence of ciclazindol on monoamine uptake and CNS function in normal subjects". Psychopharmacology.
  6. (July 1979). "Cardiovascular and autonomic actions of ciclazindol and tricyclic antidepressants". Archives Internationales de Pharmacodynamie et de Therapie.
  7. (January 1980). "The effects of mianserine, amitriptyline, ciclazindol and viloxazine on presynaptic alpha-receptors in isolated rat atria [proceedings]". British Journal of Pharmacology.
  8. (May 1992). "The involvement of potassium channels in the action of ciclazindol in rat portal vein". British Journal of Pharmacology.
  9. (April 1996). "Ciclazindol inhibits ATP-sensitive K+ channels and stimulates insulin secretion in CR1-G1 insulin-secreting cells". Molecular Pharmacology.
  10. (December 1996). "Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter". Journal of Medicinal Chemistry.
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tertiary-alcohols anorectics norepinephrine-reuptake-inhibitors 3-chlorophenyl-compounds
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