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Atlas / Drug / Isoproterenol

Isoproterenol

drug
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Also known as A-21AleudrinAludrineAsiprenolAsmalarAssiprenolBellasthmanIsonorinIsoprenalinaIsoprenalineIsopropydrinIsoproterenol dl-formIsoreninIsuprenNeo-epinineNeodrenalNovodrinNSC-33791NSC-9975

Summary

Isoproterenol (CHEMBL434) is an approved small-molecule sympathomimetic agent (ATC C01CA02) targeting ADRB1, ADRB2, and ADRB3; indicated across 7 conditions including cardiovascular disorder and obstructive lung disease.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C01CA02 (+3 more)
  • Targets: 3 (ADRB1, ADRB2, ADRB3)
  • Indications: 7 conditions
  • Clinical trials: 16
  • Chemistry: 211.26 Da · C11H17NO3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL434
NameIsoproterenol
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID3779
ChEBICHEBI:64317
ATCC01CA02, R03CB51, R03AB02, R03CB01
Molecular formulaC11H17NO3
Molecular weight211.26
InChIKeyJWZZKOKVBUJMES-UHFFFAOYSA-N

SMILES: CC(C)NCC(C1=CC(=C(C=C1)O)O)O

IUPAC name: 4-[1-hydroxy-2-(propan-2-ylamino)ethyl]benzene-1,2-diol

ChEBI definition: A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on β-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.

Pharmacological roles (ChEBI): sympathomimetic agent, β-adrenergic agonist, bronchodilator agent, cardiotonic drug.

Also known as: A-21, Aleudrin, Aludrine, Asiprenol, Asmalar, Assiprenol, Bellasthman, Isonorin, Isoprenalina, Isoprenaline, Isopropydrin, Isoproterenol

Parent form; salt/anhydrous children: CHEMBL1711, CHEMBL3989521

Patent coverage: 12,178 distinct patent families (40,234 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 40,137 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
ADRB1β1-adrenoceptorFull agonist70%P08588
ADRB2β2-adrenoceptorFull agonist6.60.4%P07550
ADRB3β3-adrenoceptorFull agonist6.20.1%P13945

Broader ChEMBL bioactivity targets: 51 (assay-derived). Sample: Microtubule-associated protein tau, 4’-phosphopantetheinyl transferase ffp, Adrenergic receptor alpha-1, Taste receptor type 2 member 31, Adrenergic receptor alpha-2, Adrenergic receptor beta, Adrenergic receptor alpha-1, Adrenergic receptor beta, Beta-2 adrenergic receptor, Beta-adrenergic receptor.

Bioactivity

ChEMBL activities: 151 potent at pChembl ≥ 5 of 163 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
ADRB110.08EC500.08nMCHEMBL_ACT_1436810
ADRB110.08EC500.08nMCHEMBL_ACT_2117342
ADRB110.08EC500.08nMCHEMBL_ACT_2374131
ADRB110.08EC500.08nMCHEMBL_ACT_2448337
ADRB110.08EC500.08nMCHEMBL_ACT_2565046
P5483310IC500.1nMCHEMBL_ACT_1181729
P5483310IC500.1nMCHEMBL_ACT_461044
P1060810IC500.1nMCHEMBL_ACT_461045
ADRB29.8EC500.16nMCHEMBL_ACT_1712410
ADRB29.8EC500.16nMCHEMBL_ACT_663635
ADRB29.7EC500.2nMCHEMBL_ACT_13871642
ADRB29.67EC500.21nMCHEMBL_ACT_23306534
ADRB29.5EC500.32nMCHEMBL_ACT_18786117
ADRB29.5EC500.32nMCHEMBL_ACT_18988265
ADRB29.33EC500.47nMCHEMBL_ACT_25928966
ADRB29.15EC500.7nMCHEMBL_ACT_18704116
ADRB19.08EC500.84nMCHEMBL_ACT_2509549
ADRB29.08EC500.84nMCHEMBL_ACT_2706017
ADRB39.01EC500.97nMCHEMBL_ACT_1436809
ADRB39.01EC500.97nMCHEMBL_ACT_2117299
ADRB39.01EC500.97nMCHEMBL_ACT_2374109
ADRB39.01EC500.97nMCHEMBL_ACT_2448335
ADRB39.01EC500.97nMCHEMBL_ACT_2509547
ADRB39.01EC500.97nMCHEMBL_ACT_2565045
ADRB19EC501nMCHEMBL_ACT_1712412
ADRB19EC501nMCHEMBL_ACT_663637
ADRB28.92EC501.2nMCHEMBL_ACT_19313174
ADRB18.9EC501.26nMCHEMBL_ACT_23306495
ADRA1D8.82EC501.5nMCHEMBL_ACT_183713
ADRB18.75EC501.78nMCHEMBL_ACT_25929010

Target pathways

Aggregated over 3 target gene(s): ADRB1, ADRB2, ADRB3.

Top Reactome pathways

16 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction3ADRB1, ADRB2, ADRB3
Signaling by GPCR3ADRB1, ADRB2, ADRB3
Class A/1 (Rhodopsin-like receptors)3ADRB1, ADRB2, ADRB3
Amine ligand-binding receptors3ADRB1, ADRB2, ADRB3
GPCR downstream signalling3ADRB1, ADRB2, ADRB3
Adrenoceptors3ADRB1, ADRB2, ADRB3
G alpha (s) signalling events3ADRB1, ADRB2, ADRB3
GPCR ligand binding3ADRB1, ADRB2, ADRB3
Membrane Trafficking1ADRB2
Metabolism of proteins1ADRB2
Vesicle-mediated transport1ADRB2
Deubiquitination1ADRB2
Ub-specific processing proteases1ADRB2
Post-translational protein modification1ADRB2
Cargo recognition for clathrin-mediated endocytosis1ADRB2
Clathrin-mediated endocytosis1ADRB2

Dominant GO biological processes

GO termTargets
diet induced thermogenesis3
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure3
adenylate cyclase-activating G protein-coupled receptor signaling pathway3
response to cold3
heat generation3
negative regulation of multicellular organism growth3
positive regulation of MAPK cascade3
brown fat cell differentiation3
adenylate cyclase-activating adrenergic receptor signaling pathway3
positive regulation of cold-induced thermogenesis3
signal transduction3
G protein-coupled receptor signaling pathway3
positive regulation of cardiac muscle cell apoptotic process2
adenylate cyclase-modulating G protein-coupled receptor signaling pathway2
negative regulation of smooth muscle contraction2

Indications & clinical

Indications

7 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
cardiovascular disorder4MONDO:0004995EFO:0000319
obstructive lung disease4MONDO:0002267HP:0006536
atrial fibrillation2MONDO:0004981EFO:0000275
nephrolithiasis2MONDO:0008171EFO:0004253
lipoma1MONDO:0005106EFO:0000759
orthostatic hypotension1MONDO:0005469EFO:0005252
postural orthostatic tachycardia syndrome1MONDO:0011479EFO:1000645

Clinical trials

Total trials: 16.

Phase distribution

PhaseTrials
Not specified9
EARLY_PHASE13
PHASE22
PHASE2/PHASE31
PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00428428PHASE2/PHASE3COMPLETEDPharmacological Modulation of the Intrarenal Pressure During Endourological Procedures in the Upper Urinary Tract
NCT00323843PHASE2UNKNOWNRetrograde Intrarenal Stone Surgery - A Method of Treating the ESWL Resistant Kidney Stone
NCT03032965PHASE2COMPLETEDAdenosine to Assess Complete Conduction Block During Catheter Ablation of Paroxysmal Atrial Fibrillation
NCT00748059PHASE1COMPLETEDThe Pathophysiology of Orthostatic Hypotension
NCT05219799EARLY_PHASE1RECRUITINGSex Disparities in Hypoxic Vasodilation and Impact of Obesity
NCT06520982EARLY_PHASE1RECRUITINGEarly Neurovascular Adaptations in Aging Women
NCT06643221EARLY_PHASE1RECRUITINGExercise as an Immune Adjuvant for Allogeneic Cell Therapies
NCT02673996Not specifiedRECRUITINGPOTS Adrenergic Ab (CIHR Aims #1&2)
NCT02725060Not specifiedENROLLING_BY_INVITATIONAutoimmune Basis for Postural Tachycardia Syndrome
NCT00226551Not specifiedCOMPLETEDVascular Response to Isoproterenol and β2 Adrenergic Receptor Polymorphisms
NCT01377636Not specifiedCOMPLETEDMeasurement of Bispectral Index and Awareness in Patients Undergoing Electrophysiology Studies With Isoproterenol
NCT02524145Not specifiedCOMPLETEDChronotropic Incompetence in Patients With HFpEF
NCT02615119Not specifiedCOMPLETEDNeural Basis of Meal Related Interoceptive Dysfunction in Anorexia Nervosa
NCT02726620Not specifiedCOMPLETEDDecision Support for Intraoperative Low Blood Pressure
NCT03019081Not specifiedUNKNOWNAugmented Interoceptive Exposure Training in Anorexia Nervosa
NCT06082388Not specifiedUNKNOWNAtropine vs Isoprenaline in the Invasive Diagnosis of Arrhythmias

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 2 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

280 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
CrizotinibChEMBL + PubChemPhase 4 (approved)ADRB1, ADRB2, ADRB3
DesloratadineChEMBL + PubChemPhase 4 (approved)ADRB1, ADRB2, ADRB3
DihydroergotamineChEMBL + PubChemPhase 4 (approved)ADRB1, ADRB2, ADRB3
PramipexoleChEMBL + PubChemPhase 4 (approved)ADRB1, ADRB2, ADRB3
RIFAMPINChEMBL + PubChemPhase 4 (approved)ADRB1, ADRB2, ADRB3
TEGASERODChEMBL + PubChemPhase 4 (approved)ADRB1, ADRB2, ADRB3
ARIPIPRAZOLEChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
BISOPROLOLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
BROMOCRIPTINEChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
CARVEDILOLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
CLOTRIMAZOLEChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
EPINEPHRINEChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
FENOTEROLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
FORMOTEROLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
LABETALOLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
LEVOBUNOLOLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
MONTELUKASTChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
NOREPINEPHRINEChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
PHENYLEPHRINEChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
PIMOZIDEChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
PINDOLOLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
PRACTOLOLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
PROPAFENONEChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
PROPRANOLOLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
SALMETEROLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
SOTALOLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
TAMOXIFENChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
THIORIDAZINEChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
TIMOLOLChEMBLPhase 4 (approved)ADRB1, ADRB2, ADRB3
ALPRENOLOLChEMBLPhase 2ADRB1, ADRB2, ADRB3
BOPINDOLOLChEMBLPhase 2ADRB1, ADRB2, ADRB3
CIMATEROLChEMBLPhase 2ADRB1, ADRB2, ADRB3
FLESTOLOLChEMBLPhase 2ADRB1, ADRB2, ADRB3
LEVISOPRENALINEChEMBLPhase 2ADRB1, ADRB2, ADRB3
LEVOPROPRANOLOLChEMBLPhase 2ADRB1, ADRB2, ADRB3
MILVETEROLChEMBLPhase 2ADRB1, ADRB2, ADRB3
RAFABEGRONChEMBLPhase 2ADRB1, ADRB2, ADRB3
SOLABEGRONChEMBLPhase 2ADRB1, ADRB2, ADRB3
TRETOQUINOLChEMBLPhase 2ADRB1, ADRB2, ADRB3
XAMOTEROLChEMBLPhase 2ADRB1, ADRB2, ADRB3
ZENIDOLOLChEMBLPhase 2ADRB1, ADRB2, ADRB3
AlogliptinPubChemApprovedADRB1, ADRB2, ADRB3
BosentanPubChemApprovedADRB1, ADRB2, ADRB3
FidaxomicinPubChemApprovedADRB1, ADRB2, ADRB3
GlycopyrrolatePubChemApprovedADRB1, ADRB2, ADRB3
LinagliptinPubChemApprovedADRB1, ADRB2, ADRB3
MethotrexatePubChemApprovedADRB1, ADRB2, ADRB3
PropoxyphenePubChemApprovedADRB1, ADRB2, ADRB3
PyrazinamidePubChemApprovedADRB1, ADRB2, ADRB3
Tiotropium Bromide MonohydratePubChemApprovedADRB1, ADRB2, ADRB3
CLOZAPINEChEMBL + PubChemPhase 4 (approved)ADRB2, ADRB3
OLANZAPINEChEMBL + PubChemPhase 4 (approved)ADRB2, ADRB3
OLODATEROLChEMBL + PubChemPhase 4 (approved)ADRB1, ADRB2
TAMSULOSINChEMBL + PubChemPhase 4 (approved)ADRB1, ADRB2
ACEBUTOLOLChEMBLPhase 4 (approved)ADRB1, ADRB2
ALBUTEROLChEMBLPhase 4 (approved)ADRB1, ADRB2
AMIODARONEChEMBLPhase 4 (approved)ADRB1, ADRB3
AMITRIPTYLINEChEMBLPhase 4 (approved)ADRB1, ADRB2
AMLODIPINEChEMBLPhase 4 (approved)ADRB2, ADRB3
ARFORMOTEROLChEMBLPhase 4 (approved)ADRB1, ADRB2

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot