Ciclazindol
 | |
| Systematic (IUPAC) name | |
|---|---|
|
10-(3-chlorophenyl)-3,4-dihydro-2H-pyrimido[1,2-a]indol-10-ol | |
| Clinical data | |
| Routes of administration | Oral |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Metabolism | Renal[1] |
| Biological half-life | ~32 hours[1] |
| Excretion | Urine, feces[1] |
| Identifiers | |
| CAS Number | 37751-39-6 |
| ATC code | none |
| PubChem | CID 37825 |
| ChemSpider | 34683 |
| UNII |
Y3I9520J7P  |
| KEGG | D03486 |
| ChEMBL | CHEMBL1192491 |
| Chemical data | |
| Formula | C17H15ClN2O |
| Molar mass | 298.77 g/mol |
| |
Ciclazindol (WY-23,409) 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
- 1 2 3 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.
- 1 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.
- ↑ Levine S (1979). "A controlled comparative trial of a new antidepressant, ciclazindol". The Journal of International Medical Research 7 (1): 1–6. PMID 369921.
- 1 2 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.
- 1 2 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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