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Dotarizine
Systematic (IUPAC) name
1-[diphenylmethyl]-4-[3-(2-phenyl-1,3-dioxolan-2-yl)propyl]piperazine
Identifiers
CAS number 84625-59-2
ATC code none
PubChem 55285
Chemical data
Formula C 29H34N2O2  
Mol. mass 442.592 g/mol
SMILES eMolecules & PubChem
Synonyms Dotarizine
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

Dotarizine is a drug used in the treatment of migraine,[1] which acts as a calcium channel blocker,[2] and also as an antagonist at the 5HT2A receptor, and to a lesser extent at the 5HT1A and 5HT2C receptors.[3][4] The anti-migraine action is thought to be due to its action as a vasodilator,[5][6] but it also has some anxiolytic effects[7] and blocks amnesia produced by electroconvulsive shock in animals.[8]

References

  1. ^ Ruiz-Nuño A, Villarroya M, Cano-Abad M, Rosado A, Balfagón G, López MG, García AG. Mechanisms of blockade by the novel migraine prophylactic agent, dotarizine, of various brain and peripheral vessel contractility. European Journal of Pharmacology. 2001 Jan 12;411(3):289-99. PMID 11164387
  2. ^ Ruiz-Nuño A, Mayorgas I, Hernández-Guijo JM, Olivares R, García AG, Gandía L. Antimigraine dotarizine blocks P/Q Ca2+ channels and exocytosis in a voltage-dependent manner in chromaffin cells. European Journal of Pharmacology. 2003 Nov 14;481(1):41-50. PMID 14637173
  3. ^ Farré M, Roset PN, Llorente M, Márquez M, Albet C, Pérez JA, Herrero E, Ortíz JA. Clinical pharmacokinetics and tolerability of dotarizine in healthy subjects after single and multiple oral administration. Methods and Findings in Experimental and Clinical Pharmacology. 1997 Jun;19(5):343-50. PMID 9379783
  4. ^ Montiel C, Herrero CJ, García-Palomero E, Renart J, García AG, Lomax RB. Serotonergic effects of dotarizine in coronary artery and in oocytes expressing 5-HT2 receptors. European Journal of Pharmacology. 1997 Aug 6;332(2):183-93. PMID 9286620
  5. ^ Kuridze N, Gajkowska B, Czernicki Z, Jurkiewicz J, Cervos-Navarro J. The effect of Dotarizine--(Ca2+ channel blocker)--on vascular reactivity and ultrastructure of cerebral capillaries in animals subjected to anoxia. Folia Neuropathologica. 1998;36(2):101-8. PMID 9757621
  6. ^ Kuridze N, Czernicki Z, Jarus-Dziedzic K, Jurkiewicz J, Cervos-Navarro J. Regional differences of cerebrovascular reactivity effected by calcium channel blocker - dotarizine. Journal of Neurological Sciences. 2000 Apr 1;175(1):13-6. PMID 10785251
  7. ^ Petkov VD, Belcheva S, Konstantinova E. Anxiolytic effects of dotarizine, a possible antimigraine drug. Methods and Findings in Experimental and Clinical Pharmacology. 1995 Dec;17(10):659-68. PMID 9053586
  8. ^ Lazarova M, Petkova B, Petkov VD. Effect of dotarizine on electroconvulsive shock or pentylenetetrazol-induced amnesia and on seizure reactivity in rats. Methods and Findings in Experimental and Clinical Pharmacology. 1995 Jan-Feb;17(1):53-8. PMID 7623521
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