Page last updated: 2024-11-06

dotarizine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

dotarizine: 5-HT2 receptor antagonist; structure in first source; active metabolite, FI 6020, detected by gas chromatography; [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

dotarizine : An N-alkylpiperazine in which the two amino hydrogens of piperazine have been replaced by diphenylmethyl and 3-(2-phenyl-1,3-dioxolan-2-yl)propyl groups. A calcium channel blocker and serotonin (5-HT2) receptor antagonist used in the treatment of migraine. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID55285
CHEMBL ID2106316
CHEBI ID138033
SCHEMBL ID333044
MeSH IDM0223191

Synonyms (29)

Synonym
dotarizine [inn]
dotarizina [spanish]
dotarizine
dotarizinum [latin]
1-(diphenylmethyl)-4-(3-(2-phenyl-1,3-dioxolan-2-yl)propyl)piperazine
piperazine, 1-(diphenylmethyl)-4-(3-(2-phenyl-1,3-dioxolan-2-yl)propyl)-
1-(diphenylmethyl)-4-[3-(2-phenyl-1,3-dioxolan-2-yl)propyl]piperazin
CHEBI:138033
1-(diphenylmethyl)-4-[3-(2-phenyl-1,3-dioxolan-2-yl)propyl]piperazine
dotarizinum
fi-6026
dotarizina
1-benzhydryl-4-[3-(2-phenyl-1,3-dioxolan-2-yl)propyl]piperazine
unii-io7663s6d3
84625-59-2
io7663s6d3 ,
CHEMBL2106316
FT-0630930
dotarizine [mi]
SCHEMBL333044
smr002530536
MLS006010920
DTXSID60233630
1-benzhydryl-4-(3-(2-phenyl-1,3-dioxolan-2-yl)propyl)piperazine
Q5299417
DB06446
irganox259
1-(diphenylmethyl)-4-[3-(2-phenyl-1,3-dioxolan-2-yl)]piperazine
1-(diphenylmethyl)-4-[3-(2-phenyl-1,3-dioxolan-2-yl)propyl]-piperazine

Research Excerpts

Overview

Dotarizine is being evaluated in clinical trials for its antimigraine and antivertigo effects. It is a new diphenylmethylpiperazine derivative with Ca2+ channel blocking properties and inhibitory effects on 5-HT2A and 5- HT2C receptors.

ExcerptReferenceRelevance
"1. Dotarizine is a novel piperazine derivative structurally related to flunarizine that is currently being evaluated in clinical trials for its antimigraine and antivertigo effects. "( Dotarizine versus flunarizine as calcium antagonists in chromaffin cells.
Albillos, A; Gandía, L; García, AG; Lara, B; López, MG; Villarroya, M, 1995
)
2.36
"Dotarizine is a new diphenylmethylpiperazine derivative with Ca2+ channel blocking properties and inhibitory effects on 5-HT2A and 5-HT2C receptors. "( Clinical pharmacokinetics and tolerability of dotarizine in healthy subjects after single and multiple oral administration.
Albet, C; Farré, M; Herrero, E; Llorente, M; Márquez, M; Ortíz, JA; Pérez, JA; Roset, PN, 1997
)
2

Toxicity

ExcerptReferenceRelevance
" No serious adverse effects to dotarizine were reported."( [Efficacy and safety of dotarizine vs. cinnarizine in the symptomatic treatment of acute balance disorders (common vertigo)].
Casamitjana, JF; Colls, A; Esteller, E; Herrero, E; Lao, X; Lluansí, J; Magriñá, C; Márquez, M; Massegur, H; Miró, N; Molá, O; Ortiz, JA; Perelló, E; Prades, J; Roca-Ribas, F; Torres, J, 1998
)
0.89

Pharmacokinetics

ExcerptReferenceRelevance
" We aimed to study the physiologic, subjective and psychomotor acute effects of oral dotarizine after single dose administration, to evaluate the tolerability and safety after multiple dosing over 2 weeks, and to study the pharmacokinetic parameters and linearity after single and multiple administration."( Clinical pharmacokinetics and tolerability of dotarizine in healthy subjects after single and multiple oral administration.
Albet, C; Farré, M; Herrero, E; Llorente, M; Márquez, M; Ortíz, JA; Pérez, JA; Roset, PN, 1997
)
0.78

Dosage Studied

ExcerptRelevanceReference
" We aimed to study the physiologic, subjective and psychomotor acute effects of oral dotarizine after single dose administration, to evaluate the tolerability and safety after multiple dosing over 2 weeks, and to study the pharmacokinetic parameters and linearity after single and multiple administration."( Clinical pharmacokinetics and tolerability of dotarizine in healthy subjects after single and multiple oral administration.
Albet, C; Farré, M; Herrero, E; Llorente, M; Márquez, M; Ortíz, JA; Pérez, JA; Roset, PN, 1997
)
0.78
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
calcium channel blockerOne of a class of drugs that acts by selective inhibition of calcium influx through cell membranes or on the release and binding of calcium in intracellular pools.
serotonergic antagonistDrugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or serotonergic agonists.
vasodilator agentA drug used to cause dilation of the blood vessels.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
N-alkylpiperazine
dioxolane
cyclic ketalA ketal in the molecule of which the ketal carbon and one or both oxygen atoms thereon are members of a ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Research

Studies (28)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's21 (75.00)18.2507
2000's6 (21.43)29.6817
2010's1 (3.57)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.96

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index19.96 (24.57)
Research Supply Index3.47 (2.92)
Research Growth Index4.13 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.96)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (6.90%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other27 (93.10%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]