Ciclazindol Routes of administration Oral ATC code Metabolism Renal[1] Elimination half-life ~32 hours[1] Excretion Urine, feces[1]
10-(3-chlorophenyl)-3,4-dihydro-2H -pyrimido[1,2-a]indol-10-ol
CAS Number PubChem CID ChemSpider UNII KEGG ChEMBL Formula C 17 H 15 Cl N 2 O Molar mass 298.77 g·mol−1 3D model (JSmol )
Clc1cccc(c1)C3(O)c4c(N2\C3=N/CCC2)cccc4
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]
See also [ ]
References [ ]
^ a b c 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 .
^ a b 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 .
^ 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 .
^ a b 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 .
^ a b 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 .
^ 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 .
^ 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 .
^ 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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