Compounds > etintidine
Page last updated: 2024-10-15

etintidine

Description

etintidine: RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135413503
CHEMBL ID2110898
SCHEMBL ID321016
SCHEMBL ID4606453
SCHEMBL ID9642425
MeSH IDM0111387

Synonyms (25)

Synonym
etintidine [inn]
etintidina [inn-spanish]
guanidine, n''-cyano-n-(2-(((5-methyl-1h-imidazol-4-yl)methyl)thio)ethyl)-n'-2-propynyl-
etintidine
guanidine, n-cyano-n'-(2-(((5-methyl-1h-imidazol-4-yl)methyl)thio)ethyl)-n''-2-propynyl-
einecs 274-036-2
etintidinum [inn-latin]
2-cyano-1-(2-(((5-methylimidazol-4-yl)methyl)thio)ethyl)-3-(2-propynyl)guanidine
etintidinum
etintidina
a60z457ssf ,
unii-a60z457ssf
69539-53-3
SCHEMBL321016
etintidine [who-dd]
SCHEMBL4606453
DTXSID40219795
n-cyano-n'-{2-[(4-methyl-5-imidazolyl)methylthio]ethyl}-n-propargylguanidine
KEDVUOWPLAHMLZ-UHFFFAOYSA-N
CHEMBL2110898
SCHEMBL9642425
n-cyano-n'-[2-[[(4-methyl-1h-imidazol-5-yl)methyl]thio]ethyl]-n''-2-propyn-1-ylguanidine
Q27273669
1-cyano-2-[2-[(5-methyl-1h-imidazol-4-yl)methylsulfanyl]ethyl]-3-prop-2-ynylguanidine
etindine

Research Excerpts

Overview

Etintidine is a competitive antagonist of histamine H2-receptors in the isolated spontaneously beating guinea-pig right atrium. Etintidine HCl is an H2 receptor antagonist under clinical trial for the treatment of duodenal ulcer diseases.

ExcerptReference
"Etintidine is a competitive antagonist of histamine H2-receptors in the isolated spontaneously beating guinea-pig right atrium with a pA2 value of 6.6 relative to values of 6.2, 6.7 and 7.3 for cimetidine, ranitidine and tiotidine, respectively. "( A comparison of some of the pharmacological properties of etintidine, a new histamine H2-receptor antagonist, with those of cimetidine, ranitidine and tiotidine.
Buyniski, JP; Cavanagh, RL; Usakewicz, JJ, 1983)
"Etintidine is a potent competitive antagonist of histamine H2-receptors. "( Pharmacological profile of etintidine, a new histamine H2-receptor antagonist.
Katz, LB; Scott, CK; Shriver, DA, 1986)
"Etintidine HCl is a potent H2-blocker. "( Etintidine-theophylline interaction study in humans.
Abels, R; Huang, SM; Leese, PT; Marinan, B; Marriott, TB; Weintraub, HS, )
"Etintidine HCl is a potent H2-blocker. "( Etintidine-propranolol interaction study in humans.
Abels, R; Huang, SM; Marinan, B; Marriott, TB; Weintraub, HS, 1987)
"Etintidine HCl is an H2 receptor antagonist which has been under clinical trial for the treatment of duodenal ulcer diseases. "( Pharmacokinetics and bioavailability of etintidine in beagle dogs: effects of routes of administration, doses, dosage forms, and chronic dosing.
Abrams, LS; Huang, SM; Marriott, TB; Weintraub, HS, )

Actions

Etintidine did not increase the frequency of micronuclei in polychromatic erythrocytes even at the dose of 50% of the LD50 at single (24 h) and chronological preparation after drug administration. Etintidine didn't increase the revertant colonies in the presence or absence of S9 mix.

ExcerptReference
"Etintidine did not increase the revertant colonies in the presence or absence of S9 mix at concentrations from 5 to 5000 micrograms/plate in either of the bacterial tester strains."( Mutagenic evaluation of etintidine (BL-5641), a novel histamine H2-receptor antagonist, using reverse mutation tests in bacteria and forward mutation tests in V79 Chinese hamster cells.
Fukushima, M; Ishida, F; Kamei, T; Kondo, H, 1987)
"(2) Etintidine did not increase the frequency of micronuclei in polychromatic erythrocytes even at the dose of 50% of the LD50 at single (24 h) and chronological preparation after drug administration."( Mutagenic evaluation of etintidine (BL-5641), a novel histamine H2-receptor antagonist, using the chromosome aberration test in CHL cells and the micronucleus test in mice.
Ishida, F; Kamei, T, 1987)

Pharmacokinetics

ExcerptReference
"The present study was designed to determine the single- and multiple-dose pharmacokinetic profiles of the H2 receptor antagonist etintidine in healthy volunteers."( Single-dose and multiple-dose pharmacokinetics of etintidine in healthy volunteers.
Abels, R; Arnold, JD; Boccagno, J; Harris, W; Huang, SM; Marriott, TB; Weintraub, HS, 1988)
" Mean Cmax (0."( Clinical pharmacokinetics of etintidine.
Abels, R; Arnold, JD; Boccagno, J; Harris, W; Huang, SM; Marriott, TB; Weintraub, HS, )

Bioavailability

Study compared etintidine from capsules (2 X 200 mg) taken under fasting conditions, with food and with milk.

ExcerptReference
"), total pepsin output, and is well absorbed from the gastrointestinal tract."( Pharmacological profile of etintidine, a new histamine H2-receptor antagonist.
Katz, LB; Scott, CK; Shriver, DA, 1986)
"A three-way crossover study was conducted in 24 normal, male volunteers to compare the bioavailability of etintidine from capsules (2 X 200 mg) taken under fasting conditions, with food and with milk."( The effect of food or milk on the bioavailability of etintidine in healthy subjects.
Abels, R; Boccagno, JA; Huang, SM; Marriott, TB; Weintraub, HS, 1988)
" Our studies are to determine the effects of routes of administration, doses, dosage forms, and chronic dosing on the bioavailability and pharmacokinetics of etintidine (E) in the beagle dog."( Pharmacokinetics and bioavailability of etintidine in beagle dogs: effects of routes of administration, doses, dosage forms, and chronic dosing.
Abrams, LS; Huang, SM; Marriott, TB; Weintraub, HS, )

Dosage Studied

ExcerptReference
" Our studies are to determine the effects of routes of administration, doses, dosage forms, and chronic dosing on the bioavailability and pharmacokinetics of etintidine (E) in the beagle dog."( Pharmacokinetics and bioavailability of etintidine in beagle dogs: effects of routes of administration, doses, dosage forms, and chronic dosing.
Abrams, LS; Huang, SM; Marriott, TB; Weintraub, HS, )
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-199020 (100.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)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 (%)
Trials8 (33.33%)5.53%
Reviews1 (4.17%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (62.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
histamine
[no description available]		3.7630aralkylamino compound;
imidazoles		human metabolite;
mouse metabolite;
neurotransmitter
cimetidine
Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach.		7.07103aliphatic sulfide;
guanidines;
imidazoles;
nitrile		adjuvant;
analgesic;
anti-ulcer drug;
H2-receptor antagonist;
P450 inhibitor
hexobarbital
Hexobarbital: A barbiturate that is effective as a hypnotic and sedative.. hexobarbital : A member of the class of barbiturates taht is barbituric acid substituted at N-1 by methyl and at C-5 by methyl and cyclohex-1-enyl groups.		1.9610barbiturates
propranolol
Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.		8.3511naphthalenes;
propanolamine;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic
edetic acid
Edetic Acid: A chelating agent that sequesters a variety of polyvalent cations such as CALCIUM. It is used in pharmaceutical manufacturing and as a food additive.		1.9710ethylenediamine derivative;
polyamino carboxylic acid;
tetracarboxylic acid		anticoagulant;
antidote;
chelator;
copper chelator;
geroprotector
dimethylnitrosamine
Dimethylnitrosamine: A nitrosamine derivative with alkylating, carcinogenic, and mutagenic properties. It causes serious liver damage and is a hepatocarcinogen in rodents.		1.9710nitrosaminegeroprotector;
mutagen
thiazoles
[no description available]		1.96101,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
dihydrotestosterone
Dihydrotestosterone: A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.. 17beta-hydroxyandrostan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4-5 double bond has been reduced to a single bond with unspecified configuration at position 5.. 17beta-hydroxy-5alpha-androstan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4,5 double bond has been reduced to a single bond with alpha-configuration at position 5.		1.961017beta-hydroxy steroid;
17beta-hydroxyandrostan-3-one;
3-oxo-5alpha-steroid		androgen;
Daphnia magna metabolite;
human metabolite;
mouse metabolite
tiotidine
tiotidine: UD gives slightly different structure for this cpd; RN given refers to parent cpd; structure in first source		6.9610thiazoles
4-hydroxypropranolol
4-hydroxypropranolol: metabolite of propanolol; RN given refers to parent cpd without isomeric designation		3.3511naphthols
nadp
[no description available]		1.9710
ranitidine
Ranitidine: A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.. ranitidine : A member of the class of furans used to treat peptic ulcer disease (PUD) and gastroesophageal reflux disease.		6.1152C-nitro compound;
furans;
organic sulfide;
tertiary amino compound		anti-ulcer drug;
drug allergen;
environmental contaminant;
H2-receptor antagonist;
xenobiotic
nad
NAD(1-) : An anionic form of nicotinamide adenine dinucleotide arising from deprotonation of the two OH groups of the diphosphate moiety.		1.9710organophosphate oxoanioncofactor;
human metabolite;
hydrogen acceptor;
Saccharomyces cerevisiae metabolite
gastrins
Gastrins: A family of gastrointestinal peptide hormones that excite the secretion of GASTRIC JUICE. They may also occur in the central nervous system where they are presumed to be neurotransmitters.		5.732
methylnitronitrosoguanidine
Methylnitronitrosoguanidine: A nitrosoguanidine derivative with potent mutagenic and carcinogenic properties.. N-methyl-N'-nitro-N-nitrosoguanidine : An N-nitroguanidine compound having nitroso and methyl substituents at the N'-position		1.9710nitroso compoundalkylating agent
ConditionIndicatedRelationship StrengthStudiesTrials
Curling Ulcer
Acute stress DUODENAL ULCER, usually observed in patients with extensive third-degree burns.		05.7442
Duodenal Ulcer
A PEPTIC ULCER located in the DUODENUM.		05.7442
Diathesis
[description not available]		02.8810
Gastroduodenal Ulcer
[description not available]		02.8810
Gastric Ulcer
[description not available]		02.8810
Peptic Ulcer
Ulcer that occurs in the regions of the GASTROINTESTINAL TRACT which come into contact with GASTRIC JUICE containing PEPSIN and GASTRIC ACID. It occurs when there are defects in the MUCOSA barrier. The common forms of peptic ulcers are associated with HELICOBACTER PYLORI and the consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).		02.8810
Stomach Ulcer
Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).		02.8810
Abnormalities, Autosome
[description not available]		01.9710
Esophagitis, Reflux
[description not available]		03.3511
Esophagitis, Peptic
INFLAMMATION of the ESOPHAGUS that is caused by the reflux of GASTRIC JUICE with contents of the STOMACH and DUODENUM.		03.3511