Dotarizine

Dotarizine
Clinical data
Other names	Dotarizine
ATC code	none;
Identifiers
	IUPAC name 1-[diphenylmethyl]-4-[3-(2-phenyl-1,3-dioxolan-2-yl)propyl]piperazine;
CAS Number	84625-59-2 ;
PubChem CID	55285;
ChemSpider	49929 ;
UNII	IO7663S6D3;
ChEBI	CHEBI:138033;
ChEMBL	ChEMBL2106316 ;
CompTox Dashboard (EPA)	DTXSID60233630 ;
Chemical and physical data
Formula	C29H34N2O2
Molar mass	442.603 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1CN(CCN1CCCC2(OCCO2)C3=CC=CC=C3)C(C4=CC=CC=C4)C5=CC=CC=C5;
	InChI InChI=1S/C29H34N2O2/c1-4-11-25(12-5-1)28(26-13-6-2-7-14-26)31-21-19-30(20-22-31)18-10-17-29(32-23-24-33-29)27-15-8-3-9-16-27/h1-9,11-16,28H,10,17-24H2 ; Key:LRMJAFKKJLRDLE-UHFFFAOYSA-N ;
	(what is this?) (verify)

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 5HT_2A receptor, and to a lesser extent at the 5HT_1A and 5HT_2C 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

^ Ruiz-Nuño A, Villarroya M, Cano-Abad M, Rosado A, Balfagón G, López MG, García AG (January 2001). "Mechanisms of blockade by the novel migraine prophylactic agent, dotarizine, of various brain and peripheral vessel contractility". European Journal of Pharmacology. 411 (3): 289–99. doi:10.1016/S0014-2999(00)00897-9. PMID 11164387.
^ Ruiz-Nuño A, Mayorgas I, Hernández-Guijo JM, Olivares R, García AG, Gandía L (November 2003). "Antimigraine dotarizine blocks P/Q Ca2+ channels and exocytosis in a voltage-dependent manner in chromaffin cells". European Journal of Pharmacology. 481 (1): 41–50. doi:10.1016/j.ejphar.2003.09.013. PMID 14637173.
^ Farré M, Roset PN, Llorente M, Márquez M, Albet C, Pérez JA, et al. (June 1997). "Clinical pharmacokinetics and tolerability of dotarizine in healthy subjects after single and multiple oral administration". Methods and Findings in Experimental and Clinical Pharmacology. 19 (5): 343–50. PMID 9379783.
^ Montiel C, Herrero CJ, García-Palomero E, Renart J, García AG, Lomax RB (August 1997). "Serotonergic effects of dotarizine in coronary artery and in oocytes expressing 5-HT2 receptors". European Journal of Pharmacology. 332 (2): 183–93. doi:10.1016/S0014-2999(97)01073-X. PMID 9286620.
^ Kuridze N, Gajkowska B, Czernicki Z, Jurkiewicz J, Cervos-Navarro J (1998). "The effect of Dotarizine--(Ca2+ channel blocker)--on vascular reactivity and ultrastructure of cerebral capillaries in animals subjected to anoxia". Folia Neuropathologica. 36 (2): 101–8. PMID 9757621.
^ Kuridze N, Czernicki Z, Jarus-Dziedzic K, Jurkiewicz J, Cervos-Navarro J (April 2000). "Regional differences of cerebrovascular reactivity effected by calcium channel blocker - dotarizine". Journal of the Neurological Sciences. 175 (1): 13–6. doi:10.1016/S0022-510X(00)00275-6. PMID 10785251. S2CID 30117433.
^ Petkov VD, Belcheva S, Konstantinova E (December 1995). "Anxiolytic effects of dotarizine, a possible antimigraine drug". Methods and Findings in Experimental and Clinical Pharmacology. 17 (10): 659–68. PMID 9053586.
^ Lazarova M, Petkova B, Petkov VD (1995). "Effect of dotarizine on electroconvulsive shock or pentylenetetrazol-induced amnesia and on seizure reactivity in rats". Methods and Findings in Experimental and Clinical Pharmacology. 17 (1): 53–8. PMID 7623521.

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[1] Ruiz-Nuño A, Villarroya M, Cano-Abad M, Rosado A, Balfagón G, López MG, García AG (January 2001). "Mechanisms of blockade by the novel migraine prophylactic agent, dotarizine, of various brain and peripheral vessel contractility". European Journal of Pharmacology. 411 (3): 289–99. doi:10.1016/S0014-2999(00)00897-9. PMID 11164387.

[2] Ruiz-Nuño A, Mayorgas I, Hernández-Guijo JM, Olivares R, García AG, Gandía L (November 2003). "Antimigraine dotarizine blocks P/Q Ca2+ channels and exocytosis in a voltage-dependent manner in chromaffin cells". European Journal of Pharmacology. 481 (1): 41–50. doi:10.1016/j.ejphar.2003.09.013. PMID 14637173.

[3] Farré M, Roset PN, Llorente M, Márquez M, Albet C, Pérez JA, et al. (June 1997). "Clinical pharmacokinetics and tolerability of dotarizine in healthy subjects after single and multiple oral administration". Methods and Findings in Experimental and Clinical Pharmacology. 19 (5): 343–50. PMID 9379783.

[4] Montiel C, Herrero CJ, García-Palomero E, Renart J, García AG, Lomax RB (August 1997). "Serotonergic effects of dotarizine in coronary artery and in oocytes expressing 5-HT2 receptors". European Journal of Pharmacology. 332 (2): 183–93. doi:10.1016/S0014-2999(97)01073-X. PMID 9286620.

[5] Kuridze N, Gajkowska B, Czernicki Z, Jurkiewicz J, Cervos-Navarro J (1998). "The effect of Dotarizine--(Ca2+ channel blocker)--on vascular reactivity and ultrastructure of cerebral capillaries in animals subjected to anoxia". Folia Neuropathologica. 36 (2): 101–8. PMID 9757621.

[6] Kuridze N, Czernicki Z, Jarus-Dziedzic K, Jurkiewicz J, Cervos-Navarro J (April 2000). "Regional differences of cerebrovascular reactivity effected by calcium channel blocker - dotarizine". Journal of the Neurological Sciences. 175 (1): 13–6. doi:10.1016/S0022-510X(00)00275-6. PMID 10785251. S2CID 30117433.

[7] Petkov VD, Belcheva S, Konstantinova E (December 1995). "Anxiolytic effects of dotarizine, a possible antimigraine drug". Methods and Findings in Experimental and Clinical Pharmacology. 17 (10): 659–68. PMID 9053586.

[8] Lazarova M, Petkova B, Petkov VD (1995). "Effect of dotarizine on electroconvulsive shock or pentylenetetrazol-induced amnesia and on seizure reactivity in rats". Methods and Findings in Experimental and Clinical Pharmacology. 17 (1): 53–8. PMID 7623521.

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