Page last updated: 2024-09-22

alinidine

Cross-References

ID SourceID
PubMed CID36354
CHEMBL ID278581
SCHEMBL ID828946
MeSH IDM0077941

Synonyms (53)

Synonym
st-567-br
alinidine
st-567
33178-86-8
n-(2,6-dichlorophenyl)-n-prop-2-en-1-yl-4,5-dihydro-1h-imidazol-2-amine
alinidin
2-(n-allyl-2,6-dichloroanilino)-2-imidazoline
2-imidazoline, 2-(n-allyl-2,6-dichloroanilino)-
2-(n-allyl-n-(2,6-dichlorophenyl)amino)-2-imidazoline
1h-imidazol-2-amine, n-(2,6-dichlorophenyl)-4,5-dihydro-n-2-propenyl-
brn 0961200
alinidina [inn-spanish]
alinidinum [inn-latin]
NCGC00162175-02
NCGC00162175-01
NCGC00162175-03
st 567 br (as hbr)
st 567-br (as hbr)
st-567-br-(as-hbr)
CHEMBL278581
st 567-br [as hydrobromide]
n-(2,6-dichlorophenyl)-n-prop-2-enyl-4,5-dihydro-1h-imidazol-2-amine
dtxsid4022571 ,
cas-33178-86-8
tox21_112002
dtxcid702571
cas_33178-86-8
bdbm85231
alinidina
alinidinum
e7idj8ds1d ,
5-25-09-00280 (beilstein handbook reference)
alinidine [inn:ban]
unii-e7idj8ds1d
n-(2,6-dichlorophenyl)-4,5-dihydro-n-2-propenyl-1h-imidazol-2-amine
LP00514
SCHEMBL828946
st 567 br (as hydrobromide)
alinidine [inn]
alinidine [mi]
alinidine [mart.]
st 567-br (as hydrobromide)
st-567-br-(as-hydrobromide)
alinidine [who-dd]
2-[n-allyl-n-(2,6-dichloro-phenyl)-amino]-2-imidazoline
allindine
n-allyl-n-(2,6-dichlorophenyl)-4,5-dihydro-1h-imidazol-2-amine #
AKOS028110641
n-allyl-n-(2,6-dichlorophenyl)-4,5-dihydro-1h-imidazol-2-amine
J-019070
FT-0713597
Q4726779
SDCCGSBI-0633723.P001

Research Excerpts

Overview

ExcerptReference
"Alinidine is a new drug which reduces heart-rate in animals by an unknown mechanism. "( Harron, DW; Riddell, JG; Shanks, RG, 1981)
"Alinidine is a new sinus node inhibitor which does not interact with the beta adrenergic receptors. "( Hugenholtz, PG; Simoons, ML, 1984)
"Alinidine is a recently developed antiarrhythmic medication that acts directly on the cardiac pacemaker cells to reduce heart rate (HR). "( Moulart, D; Preiser, JC; Vincent, JL, 1992)
"Alinidine is a new bradycardic agent that interferes with ion channels and the if pacemaker current. "( Caucheteux, D; Gurné, O; Hanet, C; Hue, L; Maldague, P; Pouleur, H; Rousseau, MF, 1989)
"Alinidine appears to be a safe drug for reduction of heart rate in patients with unstable angina and acute myocardial infarction."( Simoons, ML, 1987)
"Alinidine is a bradycardic agent, which appears to be of potential value in the therapy of coronary heart disease. "( Kreuzer, H; Wiegand, V, 1987)
"Alinidine appears to be a suitable drug for control of inappropriate sinus tachycardia in patients with heart disease undergoing surgery."( Skarvan, K, 1987)
"Alinidine is a new bradycardic agent which has been shown to be beneficial in the treatment of coronary heart disease. "( Friedrich, T; Hoffmann, M; Huckauf, H; Kammradt, G; Lichey, J, 1986)

Effects

ExcerptReference
"Alinidine has been investigated for a possible mode of action in guinea-pig atria. "( Scholtysik, G, 1982)
"Alinidine has no negative inotropic action and has no effect on the linear relation between extracellular Ca and force of myocardial contraction."( Millar, JS; Williams, EM, 1981)
"Alinidine has no beta-blocking, muscarinic or quinidine-like properties."( Friedrich, T; Hoffmann, M; Huckauf, H; Kammradt, G; Lichey, J, 1986)
"Thus alinidine has direct negative chronotropic effects, no effect on sinus node responses to sympathetic stimulation, ability to diminish sinus node and AV junctional responses to vagal stimulations without interference at the cholinergic muscarinic receptor, and 4) no effect on AV nodal conduction."( Hageman, GR; James, TN; Neely, BH; Urthaler, F, 1985)

Actions

ExcerptReference
"Alinidine did not increase resting potential or accelerate repolarisation, suggesting that potassium conductance was not increased."( Millar, JS; Williams, EM, 1981)

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
estrogen nuclear receptor alphaHomo sapiens (human)Potency11.88320.000229.305416,493.5996AID743079
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency7.94330.01789.637444.6684AID588834
DNA polymerase kappa isoform 1Homo sapiens (human)Potency23.77810.031622.3146100.0000AID588579
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (21)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID175392Dose required to decrease heart rate after iv injection to spinal rats1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Chemistry, pharmacology, and structure-activity relationships with a new type of imidazolines exerting a specific bradycardic action at a cardiac site.
AID197543Antagonistic activity in the rat thoracic aorta2001Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
Recent developments in the biology and medicinal chemistry of potassium channel modulators: update from a decade of progress.
AID24224Partition coefficient (logD7.4)1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Chemistry, pharmacology, and structure-activity relationships with a new type of imidazolines exerting a specific bradycardic action at a cardiac site.
AID189698Evaluated for decreased heart rate in spinal rats, relative activity was determined1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Chemistry, pharmacology, and structure-activity relationships with a new type of imidazolines exerting a specific bradycardic action at a cardiac site.
AID25620Dissociation constant (pKa)1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Chemistry, pharmacology, and structure-activity relationships with a new type of imidazolines exerting a specific bradycardic action at a cardiac site.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (134)

TimeframeStudies, This Drug (%)All Drugs %
pre-199092 (68.66)18.7374
1990's26 (19.40)18.2507
2000's8 (5.97)29.6817
2010's4 (2.99)24.3611
2020's4 (2.99)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 (%)
Trials22 (14.86%)5.53%
Reviews7 (4.73%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other119 (80.41%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research Highlights

Safety/Toxicity (1)

ArticleYear
Safety and efficacy of alinidine in symptom-free asthmatics.
European journal of clinical pharmacology, Volume: 31, Issue: 4
1986
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Long-term Use (2)

ArticleYear
Alinidine pharmacokinetics following acute and chronic dosing.
British journal of clinical pharmacology, Volume: 13, Issue: 6
1982
An assessment of the contribution of clonidine metabolised from alinidine to the cardiovascular effects of alinidine.
British journal of clinical pharmacology, Volume: 16, Issue: 4
1983
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (5)

ArticleYear
Proof of the linearity of the pharmacokinetics of alinidine in man.
European journal of clinical pharmacology, Volume: 21, Issue: 3
1981
Alinidine pharmacokinetics following acute and chronic dosing.
British journal of clinical pharmacology, Volume: 13, Issue: 6
1982
Effect of dobutamine on cardiac function in man: reciprocal roles of heart rate and ventricular stroke volume.
Critical care medicine, Volume: 10, Issue: 6
1982
Relative roles of heart rate and ventricular stroke volume for the regulation of cardiac output during controlled hypotension with sodium nitroprusside in man.
European journal of clinical investigation, Volume: 12, Issue: 1
1982
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioavailability (3)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, Volume: 96, Issue: 5
2019
Development and quality control of a highly sensitive radioimmunoassay for alinidine.
Journal of pharmacological methods, Volume: 6, Issue: 2
1981
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (12)

ArticleYear
Pacemaker selectivity: influence on rabbit atria of ionic environment and of alinidine, a possible anion antagonist.
Cardiovascular research, Volume: 15, Issue: 6
1981
Alinidine pharmacokinetics following acute and chronic dosing.
British journal of clinical pharmacology, Volume: 13, Issue: 6
1982
Haemodynamic effects of alinidine, a specific sinus node inhibition, in patients with unstable angina or myocardial infarction.
European heart journal, Volume: 5, Issue: 3
1984
An assessment of the contribution of clonidine metabolised from alinidine to the cardiovascular effects of alinidine.
British journal of clinical pharmacology, Volume: 16, Issue: 4
1983
Effects of alinidine on exercise-induced regional contractile dysfunction in dogs.
European journal of pharmacology, Oct-14, Volume: 130, Issue: 1-2
1986
Acute haemodynamic effects of a specific bradycardic agent in patients with coronary heart disease and impaired left ventricular function.
European heart journal, Volume: 8 Suppl L
1987
ST 567 compared with propranolol in stable angina.
European heart journal, Volume: 8 Suppl L
1987
ST 567 (alinidine) in stable angina: a comparison with metoprolol.
European heart journal, Volume: 8 Suppl L
1987
Alinidine in chronic stable angina: the effect on diastolic perfusion time.
Cardiology, Volume: 77, Issue: 4
1990
Anti-muscarinic effect of alinidine on acetylcholine-induced vasodilation in isolated and perfused dog coronary arteries.
The Tohoku journal of experimental medicine, Volume: 165, Issue: 2
1991
Addition of alinidine, a specific bradycardic agent, to dobutamine in a canine model of endotoxic shock.
Critical care medicine, Volume: 20, Issue: 8
1992
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]