Page last updated: 2024-12-06

agreal

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

Description

veralipride: used in treatment of menopausal disorders; RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID47979
CHEMBL ID2105581
CHEBI ID135600
SCHEMBL ID237519
MeSH IDM0089169

Synonyms (50)

Synonym
AC-6822
V0163
lir-1660
agreal
veralipride
D07311
agreal (tn)
veralipride (inn)
66644-81-3
NCGC00160642-01
CHEBI:135600
2,3-dimethoxy-n-[(1-prop-2-enylpyrrolidin-2-yl)methyl]-5-sulfamoylbenzamide
dtxcid4026268
dtxsid6046268 ,
tox21_111949
cas-66644-81-3
CHEMBL2105581
agradil
lir 1660
n-((1-allyl-2-pyrrolidinyl)methyl)-5-sulfamoyl-o-veratramide
veraliprida [inn-spanish]
n-((1-allyl-2-pyrrolidinylmethyl)-5-sulfamoyl-2-veratramid
n-((1-allyl-2-pyrrolidinyl)methyl)-2,3-dimethoxy-5-sulfamoylbenzamid
veraliprida
veralipridum [inn-latin]
einecs 266-435-5
unii-s7064109ud
veralipride [inn]
s7064109ud ,
veralipridum
FT-0630767
SCHEMBL237519
veralipride [mart.]
veralipride [mi]
veralipride [who-dd]
AKOS025402237
CS-6854
HY-101797
AS-74017
2,3-dimethoxy-n-{[1-(prop-2-en-1-yl)pyrrolidin-2-yl]methyl}-5-sulfamoylbenzamide
n-((1-allylpyrrolidin-2-yl)methyl)-2,3-dimethoxy-5-sulfamoylbenzamide
Q3564216
benzamide,5-(aminosulfonyl)-2,3-dimethoxy-n-[[1-(2-propenyl)-2-pyrrolidinyl]methyl]-
DB13523
lir166
( inverted exclamation marka)-veralipride
(+/-)-veralipride;lir166
D95153
()-veralipride;lir166
BV162329

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Adverse effects were acute dyskinesia (n=2) or parkinsonian syndrome, which occurred after several months or years of treatment (n=15)."( [Extrapyramidal adverse effects of veralipride (Agreal), a drug used to treat hot flushes: a propos of 17 cases].
Andréjak, M; Geslin, JM; Gras-Champel, V; Lemaire-Hurtel, AS; Masmoudi, K; Masson, H; Munier, A, 2005
)
0.58
" Adverse effects include acute dyskinesia or Parkinsonism, which may occur after many months of treatment."( The safety of veralipride.
De Leo, V; Delia, A; Faldini, E; Morgante, G; Musacchio, MC; Petraglia, F, 2006
)
0.33
" Incidence of adverse events in a Mexican population and drug compliance according to correct use were evaluated."( Safety of veralipride for the treatment of vasomotor symptoms of menopause.
Álvarez, IM; Arias, Mde J; Bonilla, MC; Campero, RA; Campos, ER; Escudero, RB; Flores, JB; González, CC; González, JH; Haro, SS; Marín, IH; Rodríguez, MA; Valencia, MH; Vargas, MA, 2014
)
0.4
"A total of 57 adverse events were registered during the 386-month treatment."( Safety of veralipride for the treatment of vasomotor symptoms of menopause.
Álvarez, IM; Arias, Mde J; Bonilla, MC; Campero, RA; Campos, ER; Escudero, RB; Flores, JB; González, CC; González, JH; Haro, SS; Marín, IH; Rodríguez, MA; Valencia, MH; Vargas, MA, 2014
)
0.4

Pharmacokinetics

ExcerptReferenceRelevance
"A pharmacokinetic study of veralipride (N-[(1-allyl-2-pyrroli dinyl)methyl]-5-sulfamoyl-o-veratramide) was performed in healthy volunteers during a chronic administration."( Pharmacokinetics of veralipride after chronic administration in humans.
Barre, J; Campistron, G; Houin, G; Jung, L; Koffell, JC; Plusquellec, Y; Rochas, MA; Staveris, S; Tillement, JP, 1988
)
0.27
"A dose-dependent pharmacokinetic study of veralipride (a new post-menopausal "hot flushes" regulator) was developed in humans after oral solution administration (100, 150, 200, and 250 mg)."( Primary dose-dependent pharmacokinetic study of veralipride.
Houin, G; Jamet, G; Jung, L; Koffel, JC; Schneider, M; Staveris, S; Tillement, JP, 1985
)
0.27
"A new procedure specific for the determination of the analytical form of the model weighting function of a complex multicomponent pharmacokinetic system with or without a shunt and time delays is described."( CXT-MAIN: a software package for determination of the analytical form of the pharmacokinetic system weighting function.
Dedík, L; Durisová, M, 1996
)
0.29

Bioavailability

ExcerptReferenceRelevance
" The effect of the number of absorption sites on absorbed amounts, on area under the curves and bioavailability is taken into account."( Pharmacokinetic compartmental model with n sites of absorption along the gastrointestinal tract.
Houin, G; Plusquellec, Y, 1994
)
0.29
" Two examples from bioavailability studies in pharmacokinetics are given."( CXT-MAIN: a software package for determination of the analytical form of the pharmacokinetic system weighting function.
Dedík, L; Durisová, M, 1996
)
0.29
" The drug concentrations were obtained by convoluting the drug absorption rate quadratic function with the drug disposition model function."( DeMonS--a new deconvolution method for estimating drug absorbed at different time intervals and/or drug disposition model parameters using a monotonic cubic spline.
Gupta, SK; Hwang, SS; Yu, Z, 1997
)
0.3
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
"Veralipride in a daily dosage of 100 mg given twenty days each month was tested in 17 patients with hot flushes."( [Value of an novel molecule, veralipride, in the treatment of menopausal disorders].
Grall, JY, 1982
)
0.26
" In these four cases, dosing recommendations were not respected."( [Extrapyramidal disorders induced by veralipride (Agreal). Apropos of 5 cases].
Andréjak, M; Chetaille, E; Decocq, G; Masmoudi, K; Mizon, JP; Rosa, A,
)
0.38
" DeMonS has been applied to (i) the griseofulvin data for estimating drug absorbed at different time intervals when the drug disposition model parameters were determined separately from intravenous data, (ii) veralipride double-peak phenomenon data to estimate simultaneously the percentage of cumulative veralipride absorbed and the veralipride disposition model parameters without reference intravenous data, (iii) a comparative bioequivalence study of gastrointestinal therapeutic system (GITS) pseudoephedrine HCI (PeHCI) controlled-release oral dosage forms when the drug disposition model parameters were not available, and (iv) estimation of both drug disposition model parameters and the absorption rate of drug from Testoderm (testosterone transdermal system) in the presence of endogenous testosterone production."( DeMonS--a new deconvolution method for estimating drug absorbed at different time intervals and/or drug disposition model parameters using a monotonic cubic spline.
Gupta, SK; Hwang, SS; Yu, Z, 1997
)
0.3
" There were 386 treatment cycles; 272 were assigned to dosing schedule 1, which included 20 days of treatment with 10 days of suspension, and 114 were assigned to dosing schedule 2, which included 5 days of treatment and 2 days of suspension."( Safety of veralipride for the treatment of vasomotor symptoms of menopause.
Álvarez, IM; Arias, Mde J; Bonilla, MC; Campero, RA; Campos, ER; Escudero, RB; Flores, JB; González, CC; González, JH; Haro, SS; Marín, IH; Rodríguez, MA; Valencia, MH; Vargas, MA, 2014
)
0.4
" For the 20 × 10 dosing schedule, the highest incidence was observed for anxiety (2."( Safety of veralipride for the treatment of vasomotor symptoms of menopause.
Álvarez, IM; Arias, Mde J; Bonilla, MC; Campero, RA; Campos, ER; Escudero, RB; Flores, JB; González, CC; González, JH; Haro, SS; Marín, IH; Rodríguez, MA; Valencia, MH; Vargas, MA, 2014
)
0.4
"Both dosing schedules show acceptable safety profiles for up to 6 months of use when used according to the contraindications in the current prescribing information for standard use (2012) and recent medical literature."( Safety of veralipride for the treatment of vasomotor symptoms of menopause.
Álvarez, IM; Arias, Mde J; Bonilla, MC; Campero, RA; Campos, ER; Escudero, RB; Flores, JB; González, CC; González, JH; Haro, SS; Marín, IH; Rodríguez, MA; Valencia, MH; Vargas, MA, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
[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]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AR proteinHomo sapiens (human)Potency29.65690.000221.22318,912.5098AID743042; AID743063
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency14.12540.01237.983543.2770AID1346984
pregnane X nuclear receptorHomo sapiens (human)Potency25.11890.005428.02631,258.9301AID1346985
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency35.48130.01789.637444.6684AID588834
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (81)

TimeframeStudies, This Drug (%)All Drugs %
pre-199047 (58.02)18.7374
1990's13 (16.05)18.2507
2000's12 (14.81)29.6817
2010's8 (9.88)24.3611
2020's1 (1.23)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 39.26

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index39.26 (24.57)
Research Supply Index4.74 (2.92)
Research Growth Index4.24 (4.65)
Search Engine Demand Index59.54 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (39.26)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials23 (25.27%)5.53%
Reviews6 (6.59%)6.00%
Case Studies18 (19.78%)4.05%
Observational1 (1.10%)0.25%
Other43 (47.25%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]