Dotarizine

Calcium channel blocker used in the treatment of migraine
  • none
Identifiers
  • 1-[diphenylmethyl]-4-[3-(2-phenyl-1,3-dioxolan-2-yl)propyl]piperazine
CAS Number
  • 84625-59-2 checkY
PubChem CID
  • 55285
ChemSpider
  • 49929 ☒N
UNII
  • IO7663S6D3
ChEBI
  • CHEBI:138033
ChEMBL
  • ChEMBL2106316 ☒N
CompTox Dashboard (EPA)
  • DTXSID60233630 Edit this at Wikidata
Chemical and physical dataFormulaC29H34N2O2Molar mass442.603 g·mol−13D model (JSmol)
  • Interactive image
  • 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 ☒N
  • Key:LRMJAFKKJLRDLE-UHFFFAOYSA-N ☒N
 ☒NcheckY (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 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 (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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Antimigraine preparations (N02C)
Analgesic/abortive
Serotonergics
Ergolines
5-HT1 agonists
Triptans
Ditans
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CGRP-R antagonists
Others
Prophylactic
Calcium channel blockers
Progestogens
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Tricyclic antidepressants
Anticonvulsants
Anti-CGRP/CGRP-R mAbs
CGRP-R antagonists
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Calcium
VDCCsTooltip Voltage-dependent calcium channels
Blockers
Activators
Potassium
VGKCsTooltip Voltage-gated potassium channels
Blockers
Activators
IRKsTooltip Inwardly rectifying potassium channel
Blockers
Activators
  • GIRKTooltip G protein-coupled inwardly rectifying potassium channel-specific: ML-297 (VU0456810)
KCaTooltip Calcium-activated potassium channel
Blockers
  • BKCa-specific: Ethanol (alcohol)
  • GAL-021
Activators
K2PsTooltip Tandem pore domain potassium channel
Blockers
Activators
Sodium
VGSCsTooltip Voltage-gated sodium channels
Blockers
Activators
ENaCTooltip Epithelial sodium channel
Blockers
Activators
  • Solnatide
ASICsTooltip Acid-sensing ion channel
Blockers
Chloride
CaCCsTooltip Calcium-activated chloride channel
Blockers
Activators
CFTRTooltip Cystic fibrosis transmembrane conductance regulator
Blockers
Activators
Unsorted
Blockers
Others
TRPsTooltip Transient receptor potential channels
  • See here instead.
LGICsTooltip Ligand gated ion channels
  • See here instead.
See also: Receptor/signaling modulators • Transient receptor potential channel modulators
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5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
  • See also: Receptor/signaling modulators
  • Adrenergics
  • Dopaminergics
  • Melatonergics
  • Monoamine reuptake inhibitors and releasing agents
  • Monoamine metabolism modulators
  • Monoamine neurotoxins
  • v
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Simple piperazines
(no additional rings)
Phenylpiperazines
Benzylpiperazines
Diphenylalkylpiperazines
(benzhydrylalkylpiperazines)
Pyrimidinylpiperazines
Pyridinylpiperazines
Benzo(iso)thiazolylpiperazines
Tricyclics
(piperazine attached via side chain)
Others/Uncategorized


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