Compounds > 2-(4,5-dihydro-1h-imidazol-2-yl)-1-methyl-1h-indole
Page last updated: 2024-11-12

2-(4,5-dihydro-1h-imidazol-2-yl)-1-methyl-1h-indole

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

Description

2-(4,5-dihydro-1H-imidazol-2-yl)-1-methyl-1H-indole: PET imaging agent for the Imidazoline2 binding site; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID13869716
CHEMBL ID41103
SCHEMBL ID9265113
MeSH IDM0575965

Synonyms (11)

Synonym
CHEMBL41103 ,
108796-88-9
1h-indole, 2-(4,5-dihydro-1h-imidazol-2-yl)-1-methyl-
2-(2-imidazolin-2-yl)-1-methyl-1h-indole
LOFCLFKSYRAAFZ-UHFFFAOYSA-N
SCHEMBL9265113
2-(4,5-dihydro-1h-imidazol-2-yl)-1-methyl-1h-indole
bdbm50226966
2-(4,5-dihydro-1h-imidazol-2-yl)-1-methylindole
bu99008
STARBLD0008923
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID132449The compound was evaluated for the antagonistic activity against clonidine-induced antinociception in mouse after po administration; ND = no data1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines.
AID1561263Displacement of [3H]2-BFI from I2IR in human brain frontal cortex assessed as binding affinity at high affinity site incubated for 45 mins by liquid scintillation spectrometry relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID1561261Displacement of [3H]2-BFI from I2IR in human brain frontal cortex assessed as binding affinity at high affinity site incubated for 45 mins by liquid scintillation spectrometry2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID35482Alpha-2 adrenergic receptor antagonistic activity in rat vas deferens vs clonidine1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines.
AID1561258Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID1561268Displacement of [3H]2-BFI from I2IR in Sprague-Dawley rat brain cortex assessed as binding affinity at high binding site incubated for 45 mins by liquid scintillation spectrometry relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID1561267Displacement of [3H]2-BFI from I2IR in Sprague-Dawley rat brain cortex assessed as binding affinity at low binding site incubated for 45 mins by liquid scintillation spectrometry2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID1561266Displacement of [3H]2-BFI from I2IR in Sprague-Dawley rat brain cortex assessed as binding affinity at high binding site incubated for 45 mins by liquid scintillation spectrometry2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID1561269Selectivity index, ratio of Ki for alpha2-AR in Sprague-Dawley rat brain cortex to Ki for I2IR in Sprague-Dawley rat brain cortex2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID1561262Displacement of [3H]2-BFI from I2IR in human brain frontal cortex assessed as binding affinity at low affinity site incubated for 45 mins by liquid scintillation spectrometry2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID1561310Selectivity ratio of Ki for alpha2-AR high binding site in human brain frontal cortex to Ki for I2IR high binding site in human brain frontal cortex2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID37078Binding affinity against alpha-2 adrenergic receptor was determined by the displacement of [3H]clonidine from rat brain cortical membranes1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (10.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (50.00)24.3611
2020's4 (40.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.11

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

MetricThis Compound (vs All)
Research Demand Index12.11 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.11)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
clonidine
Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group.		1.9710clonidine;
imidazoline
moxonidine
moxonidine: structure given in first source		2.2510organohalogen compound;
pyrimidines
prazosin
Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively.		1.9710aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
yohimbine
Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.. yohimbine : An indole alkaloid with alpha2-adrenoceptor antagonist activity. It is produced by Corynanthe johimbe and Rauwolfia serpentina.		1.9710methyl 17-hydroxy-20xi-yohimban-16-carboxylatealpha-adrenergic antagonist;
dopamine receptor D2 antagonist;
serotonergic antagonist
idazoxan
Idazoxan: A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.. idazoxan : A benzodioxine that is 2,3-dihydro-1,4-benzodioxine in which one of the hydrogens at position 2 has been replaced by a 4,5-dihydro-1H-imidazol-2-yl group.		2.4220benzodioxine;
imidazolines		alpha-adrenergic antagonist
fluorodeoxyglucose f18
Fluorodeoxyglucose F18: The compound is given by intravenous injection to do POSITRON-EMISSION TOMOGRAPHY for the assessment of cerebral and myocardial glucose metabolism in various physiological or pathological states including stroke and myocardial ischemia. It is also employed for the detection of malignant tumors including those of the brain, liver, and thyroid gland. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1162)		2.41102-deoxy-2-((18)F)fluoro-D-glucose;
2-deoxy-2-fluoro-aldehydo-D-glucose
2-(2-benzofuranyl)-2-imidazoline
2-(2-benzofuranyl)-2-imidazoline: structure given in first source		2.2510benzofurans
tracizoline
tracizoline: RN given for (R-(R*,R*))-2,3-dihydroxybutanedionate (1:1); ligand for imidazoline receptor; structure in first source		2.2510
cr4056
[no description available]		2.2510
ConditionIndicatedRelationship StrengthStudiesTrials
Ache
[description not available]		01.9710
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		01.9710
Acute Confusional Senile Dementia
[description not available]		03.2340
Alzheimer Disease
A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)		03.2340
Idiopathic Parkinson Disease
[description not available]		02.2110
Parkinson Disease
A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)		02.2110
Cognitive Decline
[description not available]		02.3110
Cognitive Dysfunction
Diminished or impaired mental and/or intellectual function.		02.3110