Page last updated: 2024-11-07

cyanopindolol

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

Cross-References

ID SourceID
PubMed CID155346
CHEMBL ID378501
CHEBI ID125406
SCHEMBL ID353756
MeSH IDM0138266

Synonyms (27)

Synonym
gtpl132
nsc707473
nsc-707473
NCI60_038172
PDSP2_001585
PDSP1_001601
PDSP1_001094
PDSP2_001078
cyanopindolol
CHEBI:125406
L000210
4-[3-(tert-butylamino)-2-hydroxypropoxy]-1h-indole-2-carbonitrile
CHEMBL378501
bdbm81499
nsc_155346
cyanopindolol(+/-)
cas_155346
1h-indole-2-carbonitrile, 4-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy)-
69906-85-0
(+-)-cyanopindolol
BRD-A47884604-001-01-7
SCHEMBL353756
sr-01000597973
SR-01000597973-1
(+/-)4-(3-t-butylamino-2-hydroxypropoxy)-1h-indole-2-carbonitrile
Q5197476
DTXSID201027570

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Lactate reduced isoproterenol-induced lipolysis in a dose-response fashion and such inhibition became significant only at 16 mmol/l lactate."( Influence of lactate on isoproterenol-induced lipolysis and beta-adrenoceptors distribution in human fat cells.
Cardone, F; Cignarelli, M; Corso, M; De Pergola, G; Di Paolo, S; Garruti, G; Giorgino, R; Nardelli, G, 1989
)
0.28
" Each antagonist alone caused smaller shifts to the right in the dose-response curve to NE and, when present simultaneously, completely abolished the NE response."( Inducible expression of beta 1- and beta 2-adrenergic receptors in rat C6 glioma cells: functional interactions between closely related subtypes.
Esbenshade, TA; Guerrero, SW; Minneman, KP; Zhong, H, 1996
)
0.29
"003 mumol kg-1 shifted to the right the dose-response curve of prenalterol for its positive chronotropic effect."( Mediation of the positive chronotropic effect of CGP 12177 and cyanopindolol in the pithed rat by atypical beta-adrenoceptors, different from beta 3-adrenoceptors.
Malinowska, B; Schlicker, E, 1996
)
0.29
" Dose-response studies showed that the potency of cyanopindolol to inhibit clearance of 5-HT was equivalent to that of the selective 5-HT reuptake inhibitor fluvoxamine."( 5-HT(1B) receptor-mediated regulation of serotonin clearance in rat hippocampus in vivo.
Daws, LC; Frazer, A; Gerhardt, GA; Gould, GG; Teicher, SD, 2000
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
indolesAny compound containing an indole skeleton.
[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 (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki0.06340.00000.667310.0000AID266006; AID266007; AID266008; AID266009; AID266010
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Beta-2 adrenergic receptorHomo sapiens (human)Kd0.00040.00000.62888.9130AID1626022; AID1626023
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (32)

Processvia Protein(s)Taxonomy
diet induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
regulation of sodium ion transportBeta-2 adrenergic receptorHomo sapiens (human)
transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-2 adrenergic receptorHomo sapiens (human)
smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
cell surface receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
endosome to lysosome transportBeta-2 adrenergic receptorHomo sapiens (human)
response to coldBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase A signalingBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of bone mineralizationBeta-2 adrenergic receptorHomo sapiens (human)
heat generationBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of multicellular organism growthBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeBeta-2 adrenergic receptorHomo sapiens (human)
bone resorptionBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIBeta-2 adrenergic receptorHomo sapiens (human)
negative regulation of smooth muscle contractionBeta-2 adrenergic receptorHomo sapiens (human)
brown fat cell differentiationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of mini excitatory postsynaptic potentialBeta-2 adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cold-induced thermogenesisBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of autophagosome maturationBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of lipophagyBeta-2 adrenergic receptorHomo sapiens (human)
cellular response to amyloid-betaBeta-2 adrenergic receptorHomo sapiens (human)
response to psychosocial stressBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of cAMP-dependent protein kinase activityBeta-2 adrenergic receptorHomo sapiens (human)
positive regulation of AMPA receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressureBeta-2 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
amyloid-beta bindingBeta-2 adrenergic receptorHomo sapiens (human)
beta2-adrenergic receptor activityBeta-2 adrenergic receptorHomo sapiens (human)
protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
adenylate cyclase bindingBeta-2 adrenergic receptorHomo sapiens (human)
potassium channel regulator activityBeta-2 adrenergic receptorHomo sapiens (human)
identical protein bindingBeta-2 adrenergic receptorHomo sapiens (human)
protein homodimerization activityBeta-2 adrenergic receptorHomo sapiens (human)
protein-containing complex bindingBeta-2 adrenergic receptorHomo sapiens (human)
norepinephrine bindingBeta-2 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
nucleusBeta-2 adrenergic receptorHomo sapiens (human)
lysosomeBeta-2 adrenergic receptorHomo sapiens (human)
endosomeBeta-2 adrenergic receptorHomo sapiens (human)
early endosomeBeta-2 adrenergic receptorHomo sapiens (human)
Golgi apparatusBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
endosome membraneBeta-2 adrenergic receptorHomo sapiens (human)
membraneBeta-2 adrenergic receptorHomo sapiens (human)
apical plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneBeta-2 adrenergic receptorHomo sapiens (human)
neuronal dense core vesicleBeta-2 adrenergic receptorHomo sapiens (human)
receptor complexBeta-2 adrenergic receptorHomo sapiens (human)
plasma membraneBeta-2 adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

Assay IDTitleYearJournalArticle
AID266007Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor.
AID266009Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor.
AID266010Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor.
AID266008Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor.
AID1626022Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.
AID266006Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor.
AID1626023Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.
AID1626024Binding affinity to inactive/G protein-uncoupled human beta2-AR by immobilized artificial membrane HPLC analysis2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.
AID1346528Human 5-HT1D receptor (5-Hydroxytryptamine receptors)1991Molecular pharmacology, Aug, Volume: 40, Issue:2
Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
AID624231Antagonists at Human 5-Hydroxytryptamine receptor 5-HT1D1991Molecular pharmacology, Aug, Volume: 40, Issue:2
Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor.
AID1346302Mouse 5-HT1B receptor (5-Hydroxytryptamine receptors)1992Proceedings of the National Academy of Sciences of the United States of America, Apr-01, Volume: 89, Issue:7
Mouse 5HT1B serotonin receptor: cloning, functional expression, and localization in motor control centers.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (237)

TimeframeStudies, This Drug (%)All Drugs %
pre-199055 (23.21)18.7374
1990's127 (53.59)18.2507
2000's42 (17.72)29.6817
2010's13 (5.49)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 (%)
Trials1 (0.40%)5.53%
Reviews3 (1.21%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other243 (98.38%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]