Compounds > sdz ens 163
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sdz ens 163

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

Description

SDZ ENS 163: a muscarinic M1 receptor agonist and M2 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID189509
CHEMBL ID313227
SCHEMBL ID10385216
MeSH IDM0203175

Synonyms (18)

Synonym
sdz ens 163
CHEMBL313227 ,
117639-11-9
3-ethyldihydro-4-(1-methyl-1h-imidazol-5-yl)methyl-2(3h)-thiophenone dihydrogen phosphate
(3s-cis)-3-ethyldihydro-4-((1-methyl-1h-imidazol-5-yl)methyl)-2(3h)-thiophenone
30iz8om3kp ,
unii-30iz8om3kp
ens 213-163
2(3h)-thiophenone, 3-ethyldihydro-4-((1-methyl-1h-imidazol-5-yl)methyl)-, (3s-cis)-
bdbm50008070
3-ethyl-4-(3-methyl-3h-imidazol-4-ylmethyl)-dihydro-thiophen-2-one
(3s,4r)-3-ethyl-4-[(3-methylimidazol-4-yl)methyl]thiolan-2-one
SCHEMBL10385216
sdz-ens-163 free base
2(3h)-thiophenone, 3-ethyldihydro-4-((1-methyl-1h-imidazol-5-yl)methyl)-, (3s,4r)-
DTXSID40922494
3-ethyl-4-[(1-methyl-1h-imidazol-5-yl)methyl]thiolan-2-one
(3s,4r)-3-ethyl-4-((1-methyl-1h-imidazol-5-yl)methyl)dihydrothiophen-2(3h)-one

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" In contrast, the absorption rate of the poorly water soluble drug increased with higher dose volumes, whereas no changes in the extent of absorption were observed."( The effect of oral dose volume on the absorption of a highly and a poorly water-soluble drug in the rat.
Nickerson, DF; Tse, FL; Weaver, ML, 1994)		0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC50 (µMol)0.33980.00052.773925.1700AID141540; AID141554
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC50 (µMol)0.05400.00052.891925.1700AID141540
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC50 (µMol)0.05400.00052.747825.1700AID141540
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC50 (µMol)0.05400.00052.780225.1700AID141540
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC50 (µMol)0.05400.00053.314249.5000AID141540
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID140934Central presynaptic activity as effect on electrically evoked acetylcholine release from rat hippocampal slices (M2 model)1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.
AID193266Neuronal postsynaptic muscarinic activity was measured relative to muscurine (100%)1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.
AID101732Peripheral postsynaptic muscarinic activity was measured relative to muscarine (100%)1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.
AID141554Ability to displace [3H]pirenzepine (pir) from muscarinic acetylcholine receptor M1 in rat cortical tissue.1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.
AID197332Neuronal postsynaptic muscarinic activity was measured by firing rate of the rat hippocampal CA1 neurons in M1 model1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.
AID141540Ability to displace [3H]cis--2-methyl-5-((dimethylamino)methyl)-1,3-di oxolane from muscarinic acetylcholine receptor in rat cortical tissue.1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.
AID193265Central postsynaptic muscarinic activity was measured relative to muscurine (100%)1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.
AID197176Central postsynaptic muscarinic activity was measured by slow depolarization of the rat cervical ganglion in M1 model1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.
AID141848Ratio of ability to displace pirenzpine compared to ability to displace CD (non-selective muscarinic agonist).1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.
AID101734Peripheral postsynaptic muscarinic activity by contraction of the guinea pig ileum.1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Muscarinic activity of the thiolactone, lactam, lactol, and thiolactol analogues of pilocarpine and a hypothetical model for the binding of agonists to the m1 receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's6 (100.00)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 (%)
Trials1 (16.67%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
arecoline
Arecoline: An alkaloid obtained from the betel nut (Areca catechu), fruit of a palm tree. It is an agonist at both muscarinic and nicotinic acetylcholine receptors. It is used in the form of various salts as a ganglionic stimulant, a parasympathomimetic, and a vermifuge, especially in veterinary practice. It has been used as a euphoriant in the Pacific Islands.. arecoline : A tetrahydropyridine that is 1,2,5,6-tetrahydropyridine with a methyl group at position 1, and a methoxycarbonyl group at position 3. An alkaloid found in the areca nut, it acts as an agonist of muscarinic acetylcholine.		1.9810enoate ester;
methyl ester;
pyridine alkaloid;
tetrahydropyridine		metabolite;
muscarinic agonist
5-methylfurtrethonium
5-methylfurtrethonium: RN given refers to parent cpd; structure		1.9810aralkylamine
oxotremorine
Oxotremorine: A non-hydrolyzed muscarinic agonist used as a research tool.		1.9810N-alkylpyrrolidine
carbachol
Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.		1.9810ammonium salt;
carbamate ester		cardiotonic drug;
miotic;
muscarinic agonist;
nicotinic acetylcholine receptor agonist;
non-narcotic analgesic
pilocarpine
Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine.		7.3820pilocarpineantiglaucoma drug
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		4.4651mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
muscarine
Muscarine: A toxic alkaloid found in Amanita muscaria (fly fungus) and other fungi of the Inocybe species. It is the first parasympathomimetic substance ever studied and causes profound parasympathetic activation that may end in convulsions and death. The specific antidote is atropine.		1.9810monosaccharide
abecarnil
[no description available]		1.9810
n-methylscopolamine
N-Methylscopolamine: A muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors.		1.9810
scopolamine hydrobromide
[no description available]		3.3711
ConditionIndicatedRelationship StrengthStudiesTrials
Cognition Disorders
Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment.		03.3711