Page last updated: 2024-12-06

alinidine

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

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

Alinidine is a recently developed antiarrhythmic medication that acts directly on the cardiac pacemaker cells to reduce heart rate (HR) Alinidine appears to be a safe drug for reduction of heart rate in patients with unstable angina and acute myocardial infarction.

ExcerptReferenceRelevance
"Alinidine is a new drug which reduces heart-rate in animals by an unknown mechanism. "( Alinidine reduces heart-rate without blockade of beta-adrenoceptors.
Harron, DW; Riddell, JG; Shanks, RG, 1981
)
3.15
"Alinidine is a new sinus node inhibitor which does not interact with the beta adrenergic receptors. "( Haemodynamic effects of alinidine, a specific sinus node inhibition, in patients with unstable angina or myocardial infarction.
Hugenholtz, PG; Simoons, ML, 1984
)
2.02
"Alinidine is a recently developed antiarrhythmic medication that acts directly on the cardiac pacemaker cells to reduce heart rate (HR). "( Addition of alinidine, a specific bradycardic agent, to dobutamine in a canine model of endotoxic shock.
Moulart, D; Preiser, JC; Vincent, JL, 1992
)
2.11
"Alinidine is a new bradycardic agent that interferes with ion channels and the if pacemaker current. "( Effects of alinidine on metabolic response to high-demand myocardial ischemia.
Caucheteux, D; Gurné, O; Hanet, C; Hue, L; Maldague, P; Pouleur, H; Rousseau, MF, 1989
)
2.11
"Alinidine appears to be a safe drug for reduction of heart rate in patients with unstable angina and acute myocardial infarction."( Effect of ST-567 (a specific bradycardiac agent) in patients with unstable angina and myocardial infarction.
Simoons, ML, 1987
)
0.99
"Alinidine is a bradycardic agent, which appears to be of potential value in the therapy of coronary heart disease. "( Acute haemodynamic effects of a specific bradycardic agent in patients with coronary heart disease and impaired left ventricular function.
Kreuzer, H; Wiegand, V, 1987
)
1.72
"Alinidine appears to be a suitable drug for control of inappropriate sinus tachycardia in patients with heart disease undergoing surgery."( Value of a specific bradycardic agent in cardiac surgery compared to placebo.
Skarvan, K, 1987
)
0.99
"Alinidine is a new bradycardic agent which has been shown to be beneficial in the treatment of coronary heart disease. "( Safety and efficacy of alinidine in symptom-free asthmatics.
Friedrich, T; Hoffmann, M; Huckauf, H; Kammradt, G; Lichey, J, 1986
)
2.02

Effects

Alinidine has no negative inotropic action and has no effect on the linear relation between extracellular Ca and force of myocardial contraction. It has been investigated for a possible mode of action in guinea-pig atria.

ExcerptReferenceRelevance
"Alinidine has been investigated for a possible mode of action in guinea-pig atria. "( Inhibition of positive chronotropic effects of PGE2 by alinidine.
Scholtysik, G, 1982
)
1.95
"Alinidine has no negative inotropic action and has no effect on the linear relation between extracellular Ca and force of myocardial contraction."( Pacemaker selectivity: influence on rabbit atria of ionic environment and of alinidine, a possible anion antagonist.
Millar, JS; Williams, EM, 1981
)
1.21
"Alinidine has no beta-blocking, muscarinic or quinidine-like properties."( Safety and efficacy of alinidine in symptom-free asthmatics.
Friedrich, T; Hoffmann, M; Huckauf, H; Kammradt, G; Lichey, J, 1986
)
1.3
"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."( Negative chronotropic and parasympatholytic effects of alinidine on canine sinus node and AV junction.
Hageman, GR; James, TN; Neely, BH; Urthaler, F, 1985
)
0.97

Actions

ExcerptReferenceRelevance
"Alinidine did not increase resting potential or accelerate repolarisation, suggesting that potassium conductance was not increased."( Pacemaker selectivity: influence on rabbit atria of ionic environment and of alinidine, a possible anion antagonist.
Millar, JS; Williams, EM, 1981
)
1.21

Pharmacokinetics

ExcerptReferenceRelevance
" 2 After acute oral administration the following values were obtained; Cmax -- 166."( Alinidine pharmacokinetics following acute and chronic dosing.
Arndts, D; Harron, DW; Shanks, RG, 1982
)
1.71
" Independent of the route of administration and of the doses given, similar pharmacokinetic parameters were calculated for each group and each trial."( Proof of the linearity of the pharmacokinetics of alinidine in man.
Arndts, D; Justus, H; Rominger, KL; Warnkross, H, 1981
)
0.52

Bioavailability

ExcerptReferenceRelevance
" The bioavailability following oral administration was nearly complete (0."( Pharmacokinetic and pharmacodynamic properties of alinidine in man.
Jähnchen, E; Kasper, W; Meinertz, T; Stützle, U; Wiegand, UW,
)
0.38
" From the accumulated renally-excreted total radioactivities, the enteral absorption of the drug was calculated (91%); the bioavailability of orally administered alinidine was derived from the corresponding areas under the blood plasma concentration curves of the radioimmunologically-evaluated parent compound (72%)."( Development and quality control of a highly sensitive radioimmunoassay for alinidine.
Arndts, D; Stähle, H, 1981
)
0.69
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Alinidine does not block the positive chronotropic action of isoprenaline. Alinidine shifted the dose-response curves of acetylcholine and carbachol to the right. It did not affect those for isosorbide dinitrate, isoproterenol and adenosine.

ExcerptRelevanceReference
" Thirty minutes later, alinidine was administered as a bolus dosage of 1 mg/kg in five dogs; the other five dogs served as a control group."( Addition of alinidine, a specific bradycardic agent, to dobutamine in a canine model of endotoxic shock.
Moulart, D; Preiser, JC; Vincent, JL, 1992
)
0.97
" Alinidine (10(-6) M) shifted the dose-response curves of acetylcholine and carbachol to the right, but it did not affect those for isosorbide dinitrate, isoproterenol and adenosine."( Anti-muscarinic effect of alinidine on acetylcholine-induced vasodilation in isolated and perfused dog coronary arteries.
Chiba, S; Furukawa, Y; Nakane, T, 1991
)
1.49
" Alinidine was administered at a dosage of 30 mg 3 times a day."( Alinidine in chronic stable angina: the effect on diastolic perfusion time.
Cinquegrana, G; Condorelli, M; Duilio, C; Ferro, G; Spadafora, M; Spinelli, L, 1990
)
2.63
" It seems probable that the optimal dose of alinidine was not used in this trial and that the dosage could have been higher."( ST 567 (alinidine) in stable angina: a comparison with metoprolol.
Balakumaran, K; Bokslag, M; Fels, PW; Hugenholtz, PG; Jovanovic, A; Lubsen, J; van Es, GA, 1987
)
0.97
" We conclude that administration of alinidine in the dosage used does not lead to a significant deterioration even in patients with strongly impaired left ventricular function."( Acute haemodynamic effects of a specific bradycardic agent in patients with coronary heart disease and impaired left ventricular function.
Kreuzer, H; Wiegand, V, 1987
)
0.55
" After 2 control runs which had induced regional contractile dysfunction of comparable intensity, alinidine was infused intravenously at a dosage of 1 mg/kg per 5 min."( Effects of alinidine on exercise-induced regional contractile dysfunction in dogs.
Krumpl, G; Mayer, N; Raberger, G; Schneider, W, 1986
)
0.88
" The dose-response relation between alinidine and frequency is not altered by atropine, and alinidine does not block the positive chronotropic action of isoprenaline."( Pacemaker selectivity: influence on rabbit atria of ionic environment and of alinidine, a possible anion antagonist.
Millar, JS; Williams, EM, 1981
)
0.77
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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]

Market Indicators

Research Demand Index: 19.64

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

MetricThis Compound (vs All)
Research Demand Index19.64 (24.57)
Research Supply Index5.14 (2.92)
Research Growth Index4.20 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.64)

All Compounds (24.57)

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]