alinidine
Cross-References
ID Source | ID |
---|---|
PubMed CID | 36354 |
CHEMBL ID | 278581 |
SCHEMBL ID | 828946 |
MeSH ID | M0077941 |
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.
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.
Excerpt | Reference | Relevance |
---|---|---|
"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
Excerpt | Reference | Relevance |
---|---|---|
"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
Excerpt | Reference | Relevance |
---|---|---|
" 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
Excerpt | Reference | Relevance |
---|---|---|
" 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.
Excerpt | Relevance | Reference |
---|---|---|
" 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 |
Protein Targets (3)
Potency Measurements
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 11.8832 | 0.0002 | 29.3054 | 16,493.5996 | AID743079 |
potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 7.9433 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 23.7781 | 0.0316 | 22.3146 | 100.0000 | AID588579 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Bioassays (21)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The 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. |
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
AID175392 | Dose required to decrease heart rate after iv injection to spinal rats | 1980 | Journal 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. |
AID197543 | Antagonistic activity in the rat thoracic aorta | 2001 | Journal 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. |
AID24224 | Partition coefficient (logD7.4) | 1980 | Journal 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. |
AID189698 | Evaluated for decreased heart rate in spinal rats, relative activity was determined | 1980 | Journal 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. |
AID25620 | Dissociation constant (pKa) | 1980 | Journal 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)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 92 (68.66) | 18.7374 |
1990's | 26 (19.40) | 18.2507 |
2000's | 8 (5.97) | 29.6817 |
2010's | 4 (2.99) | 24.3611 |
2020's | 4 (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.
| This Compound (19.64) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 22 (14.86%) | 5.53% |
Reviews | 7 (4.73%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 119 (80.41%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |