Page last updated: 2024-11-06

pirenzepine dihydrochloride

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

Pirenzepine dihydrochloride is a selective muscarinic acetylcholine receptor antagonist, particularly targeting the M1 subtype. It was synthesized in the 1970s and has been studied extensively for its potential therapeutic applications. Pirenzepine dihydrochloride is known to exhibit anticholinergic effects, impacting the central and peripheral nervous systems. It has been investigated for its potential benefits in conditions such as peptic ulcers, irritable bowel syndrome, and Alzheimer's disease. Pirenzepine dihydrochloride's selectivity for M1 receptors has led to research exploring its potential as a treatment for cognitive impairment associated with dementia. However, its clinical use has been limited due to its potential side effects, including dry mouth, blurred vision, and urinary retention. Research continues to explore its therapeutic potential and explore ways to optimize its use.'

Cross-References

ID SourceID
PubMed CID71405
CHEMBL ID1531864
SCHEMBL ID41704
MeSH IDM0475054

Synonyms (78)

Synonym
einecs 249-907-5
5,11-dihydro-11-((4-methyl-1-piperazinyl)acetyl)-6h-pyrido(2,3-b)(1,4)benzodiazepin-6-one dihydrochloride
tabe
6h-pyrido(2,3-b)(1,4)benzodiazepin-6-one, 5,11-dihydro-11-((4-methyl-1-piperazinyl)acetyl)-, dihydrochloride
ls 519 cl2
pirenzepine hydrochloride [usan:jan]
leblon
ls 519cl2
maghen
6,11-dihydro-11-((4-methyl-1-piperazinyl)acetyl)-5h-pyrido(2,3-b)(1,4)benzodiazepin-6-on dihydrochlorid
ls 519 dihydrochloride
bisvanil
5,11-dihydro-11-((4-methylpiperazin-1-yl)acetyl)-6h-pyrido(2,3-b)(1,4)benzodiazepin-6-one dihydrochloride
EU-0100962
pirenzepine dihydrochloride, >=98% (tlc), powder
pirenzepine hydrochloride
pirenzepine dihydrochloride
PRESTWICK_400
29868-97-1
D01297
pirenzepine hydrochloride (usan)
NCGC00094263-02
NCGC00094263-03
SPECTRUM1501138
NCGC00094263-01
[(4-methyl-1-piperazinyl)acetyl]-6h-pyrido[2,3-b][1,4]benzodiazepin-6-one dihydrochloride
5,11-dihydro-11-
P 7412
ls519
ls 519
HMS1568I20
HMS1921J05
nsc-757846
CHEMBL1531864
ls-519 cl2
ls 519 c12
ls-519cl2
S3662
CCG-38974
pirenzepine hcl
unii-10ym403fls
10ym403fls ,
nsc 757846
FT-0619757
pirenzepine 2hcl
LP00962
5,11-dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6h-pyrido[2,3-b][1,4]benzodiazepin-6-one dihydrochloride
pirenzepine hydrochloride [mart.]
pirenzepine dihydrochloride [mi]
pirenzepine hydrochloride [vandf]
pirenzepine hydrochloride [usan]
pirenzepine dihydrochloride [who-dd]
SCHEMBL41704
tox21_500962
NCGC00261647-01
pirenzepinehydrochloride
AKOS024456369
SR-01000000220-2
sr-01000000220
11-(2-(4-methylpiperazin-1-yl)acetyl)-5h-benzo[e]pyrido[3,2-b][1,4]diazepin-6(11h)-one dihydrochloride
SR-01000000220-4
J-017673
SR-01000000220-7
FFNMBRCFFADNAO-UHFFFAOYSA-N
11-(2-(4-methylpiperazin-1-yl)acetyl)-5,11-dihydro-6h-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one dihydrochloride
pirenzepine (dihydrochloride)
CS-6975
HY-17037
pirenzepine, dihydrochloride
29868-97-1 (2hcl)
Q27114749
AS-15182
BCP12435
A51065
11-[2-(4-methyl-1-piperazinyl)-1-oxoethyl]-5h-pyrido[2,3-b][1,4]benzodiazepin-6-one hydrate hcl
DTXSID50952328
11-[2-(4-methylpiperazin-1-yl)acetyl]-5h-pyrido[2,3-b][1,4]benzodiazepin-6-one;dihydrochloride
P2457
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
hydrochlorideA salt formally resulting from the reaction of hydrochloric acid with an organic base.
[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 (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency28.18380.003245.467312,589.2998AID1705
thioredoxin reductaseRattus norvegicus (Norway rat)Potency1.12200.100020.879379.4328AID588453
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency2.66030.001530.607315,848.9004AID1224821
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency56.23410.035520.977089.1251AID504332
DNA polymerase eta isoform 1Homo sapiens (human)Potency0.17780.100028.9256213.3130AID588591
gemininHomo sapiens (human)Potency35.48130.004611.374133.4983AID463097
lamin isoform A-delta10Homo sapiens (human)Potency22.38720.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (14.29)29.6817
2010's5 (71.43)24.3611
2020's1 (14.29)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.95

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 Index21.95 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.95)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]