Page last updated: 2024-11-10

dinapsoline

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

Description

dinapsoline: a dopamine D(1) agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9816455
CHEMBL ID124561
SCHEMBL ID16938669
MeSH IDM0257110

Synonyms (17)

Synonym
dinapsoline, (r)(+)
bdbm50117181
(s)-2,3,7,11b-tetrahydro-1h-dibenzo[de,h]isoquinoline-8,9-diol
CHEMBL124561 ,
458563-40-1
dinapsoline
SCHEMBL16938669
DTXSID50431229
Q5277944
ZQTSNGJHMUKLOM-ZDUSSCGKSA-N
unii-gz9xc6c5p9
GZ9XC6C5P9 ,
8,9-dihydroxy-2,3,7,11b-tetrahydro-1h-naph(1,2,3-de)isoquinoline
(-)-(r)-dinapsoline
1h-dibenz(de,h)isoquinoline-8,9-diol, 2,3,7,11b-tetrahydro-, (11br)-
679433-68-2
(1s)-15-azatetracyclo[7.7.1.02,7.013,17]heptadeca-2(7),3,5,9(17),10,12-hexaene-5,6-diol

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Daily dosing with A-77636 rapidly produced complete tolerance, as previously observed, whereas coadministration of the D2 agonist quinpirole plus A-77636 failed to either delay or prevent tolerance."( Dinapsoline: characterization of a D1 dopamine receptor agonist in a rat model of Parkinson's disease.
Gulwadi, AG; Korpinen, CD; Mailman, RB; Nichols, DE; Sit, SY; Taber, MT, 2001
)
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)
Tryptophan 5-hydroxylase 1Rattus norvegicus (Norway rat)IC50 (µMol)0.03800.03801.30806.4300AID64427
DRattus norvegicus (Norway rat)IC50 (µMol)0.03300.00030.50267.7625AID61182
D(2) dopamine receptorRattus norvegicus (Norway rat)IC50 (µMol)0.03800.00010.54948.4000AID64427
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DRattus norvegicus (Norway rat)K 0.50.00590.00040.00420.0062AID61343
DRattus norvegicus (Norway rat)K0.50.00590.00030.01430.1490AID61346
D(2) dopamine receptorRattus norvegicus (Norway rat)K 0.50.10260.00020.47472.2500AID61330; AID64778
D(2) dopamine receptorRattus norvegicus (Norway rat)K0.50.03130.00090.02480.0581AID64780
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID202341In vitro adenylate cyclase response in neuroblastoma cell line2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist.
AID61343Inhibition of [3H]SCH-23390 binding to rat striatal membrane Dopamine receptor D11999Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
Synthesis and dopaminergic properties of benzo-fused analogues of quinpirole and quinelorane.
AID64778Inhibition of [3H]spiperone binding to rat striatal membrane Dopamine receptor D21999Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
Synthesis and dopaminergic properties of benzo-fused analogues of quinpirole and quinelorane.
AID196019In vivo number of rotations at a dose of 2 mg/kg administered subcutaneously to Sprague-Dawley rats2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist.
AID61330Affinity on C6 glioma cells transfected with Dopamine receptor D2L1999Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
Synthesis and dopaminergic properties of benzo-fused analogues of quinpirole and quinelorane.
AID227603In vitro intrinsic activity which is the ratio of the cyclase response of compound relative to that of dopamine2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist.
AID64780Binding affinity against Dopamine receptor D2 using radioligand [3H]spiperone binding assay in rat cortical membranes1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
9-Dihydroxy-2,3,7,11b-tetrahydro-1H-naph[1,2,3-de]isoquinoline: a potent full dopamine D1 agonist containing a rigid-beta-phenyldopamine pharmacophore.
AID233475Hill slope was determined for the compound in D2 receptor binding assay1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
9-Dihydroxy-2,3,7,11b-tetrahydro-1H-naph[1,2,3-de]isoquinoline: a potent full dopamine D1 agonist containing a rigid-beta-phenyldopamine pharmacophore.
AID64427In vitro inhibition of [125I]7-OH-PIPAT binding to Dopamine receptor D2 of rat striatal membrane2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist.
AID61182In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist.
AID233473Hill slope was determined for the compound in D1 receptor binding assay1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
9-Dihydroxy-2,3,7,11b-tetrahydro-1H-naph[1,2,3-de]isoquinoline: a potent full dopamine D1 agonist containing a rigid-beta-phenyldopamine pharmacophore.
AID61346Binding affinity of compound towards Dopamine receptor D1 was determined in rat striatal homogenate using [3H]SCH-23390 as radioligand1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
9-Dihydroxy-2,3,7,11b-tetrahydro-1H-naph[1,2,3-de]isoquinoline: a potent full dopamine D1 agonist containing a rigid-beta-phenyldopamine pharmacophore.
AID196018In vivo number of rotations at a dose of 0.2 mg/kg administered subcutaneously to Sprague-Dawley rats2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
(+)-Dinapsoline: an efficient synthesis and pharmacological profile of a novel dopamine agonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (22.22)18.2507
2000's7 (77.78)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]

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%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]