Page last updated: 2024-12-05

szl 49

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

Description

SZL 49: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4892
CHEMBL ID429379
MeSH IDM0146057

Synonyms (19)

Synonym
107021-36-3
szl 49
L003498
CHEMBL429379 ,
prazobind
FT-0674000
piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(bicyclo(2.2.2)octa-2,5-dien-2-ylcarbonyl)-
szl-49
1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-bicyclo(2.2.2)octa-2,5-dienylcarbonyl)piperazine
methanone,[4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl]bicyclo[2.2.2]octa-2,5-dien-2-yl-
J-001691
AKOS030255794
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(2-bicyclo[2.2.2]octa-2,5-dienyl)methanone
FT-0674001
bdbm50227880
(bicyclo[2.2.2]octa-2,5-dien-2-yl)[4-(4-imino-6,7-dimethoxy-3,4-dihydroquinazolin-2-yl)piperazin-1-yl]methanone
DTXSID80910214
HY-118335
CS-0065710

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" In control aortic rings the dose-response curves for either clonidine or naphazoline were biphasic, consisting of high- and low-affinity components."( Interaction of imidazolines with alkylation-sensitive and -resistant alpha-1 adrenoceptor subtypes.
Piascik, MT; Pruitt, TA; Sparks, MS, 1991
)
0.28
"1-10 nM) shifted the dose-response curves for norepinephrine and phenylephrine to the right."( Agonist interaction with alkylation-sensitive and -resistant alpha-1 adrenoceptor subtypes.
Butler, BT; Kusiak, JW; Piascik, MT; Pruitt, TA, 1990
)
0.28
" The phenylephrine dose-response curves for mean arterial blood pressure and total peripheral vascular resistance were shifted to the right but the maximal responses were not decreased."( Alpha 1-adrenoceptor subtypes and the regulation of peripheral hemodynamics in the conscious rat.
Barron, KW; Kusiak, JW; Piascik, MT, 1990
)
0.28
"5 hr washout, shifted to the right in a dose-dependent manner the dose-response curves for phenylephrine and norepinephrine."( Interaction of a chemically reactive prazosin analog with alpha-1 adrenoceptors of rat tissues.
Kusiak, JW; Piascik, MT; Pitha, J, 1989
)
0.28
"5 mg/kg and greater) shifted the phenylephrine dose-response curve to the right."( Effect of an alkylating analog of prazosin on alpha-1 adrenoceptor subtypes and arterial blood pressure.
Butler, BT; Holtman, JR; Kusiak, JW; Piascik, MT; Pitha, J, 1989
)
0.28
" The inhibition, which was dose and time dependent, was characterized by progressive shift to the right in the norepinephrine dose-response curve."( Alkylation of alpha-1 receptors with a chemically reactive analog of prazosin reveals low affinity sites for norepinephrine in rabbit aorta.
Babich, M; Butler, BT; Kusiak, JW; Le, HT; Piascik, MT; Pitha, J, 1988
)
0.27
" The competitive alpha1-adrenoceptor antagonists produced dextral shifts of the dose-response curves to NA in longitudinal and circular muscle."( Discrimination by SZL49 between contractions evoked by noradrenaline in longitudinal and circular muscle of human vas deferens.
Amobi, NI; Guillebaud, J; Kaisary, AV; Smith, IC; Turner, E, 2002
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00760.00021.874210.0000AID36446
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00760.00021.270410.0000AID36446
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00760.00001.819410.0000AID36446
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID36573Irreversible action on rat cerebral cortical membrane Alpha-1 adrenergic receptor at 100 nM1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Alkylating prazosin analogue: irreversible label for alpha 1-adrenoceptors.
AID36446Compound is evaluated for its ability to compete with [3H]prazosin for binding to Alpha-1 adrenergic receptor sites on rat cerebral cortical membranes at 10 nM concentration1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Alkylating prazosin analogue: irreversible label for alpha 1-adrenoceptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (29.41)18.7374
1990's10 (58.82)18.2507
2000's2 (11.76)29.6817
2010's0 (0.00)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: 11.50

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

MetricThis Compound (vs All)
Research Demand Index11.50 (24.57)
Research Supply Index2.89 (2.92)
Research Growth Index4.39 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]