Page last updated: 2024-09-25

brl 44408

Description

BRL 44408: has selectivity for adrenergic alpha-2A receptors; BRL 48962 is the R-enantiomer; BRL 48553 is the R-enantiomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID121850
CHEMBL ID216097
SCHEMBL ID7596949
MeSH IDM0195544

Synonyms (25)

Synonym
gtpl525
PDSP2_001727
PDSP1_001744
brl44408
NCGC00025023-02
2-((4,5-dihydro-1h-imidazol-2-yl)methyl)-2,3-dihydro-1-methyl-1h-isoindole
brl 44408
brl-44408
1h-isoindole, 2-((4,5-dihydro-1h-imidazol-2-yl)methyl)-2,3-dihydro-1-methyl-
2-(2h-(1-methyl-1,3-dihydroisoindole)methyl)-4,5-dihydroimidazole
CHEMBL216097
L000144
FT-0663603
2-(4,5-dihydro-1h-imidazol-2-ylmethyl)-1-methyl-1,3-dihydroisoindole
cas_121850
bdbm82520
nsc_121850
118343-19-4
zet7b198w2 ,
unii-zet7b198w2
SCHEMBL7596949
J-003739
2-[(4,5-dihydro-1h-imidazol-2-yl)methyl]-1-methyl-2,3-dihydro-1h-isoindole
DTXSID30922665
Q4836377

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RGS12Homo sapiens (human)Potency44.66840.794310.991425.1189AID2390
Microtubule-associated protein tauHomo sapiens (human)Potency31.62280.180013.557439.8107AID1460
regulator of G-protein signaling 4Homo sapiens (human)Potency1.68340.531815.435837.6858AID504845
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency22.38720.035520.977089.1251AID504332
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID1346049Human alpha2A-adrenoceptor (Adrenoceptors)1994The Journal of pharmacology and experimental therapeutics, Dec, Volume: 271, Issue:3
The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.
AID1346058Human alpha2B-adrenoceptor (Adrenoceptors)1994The Journal of pharmacology and experimental therapeutics, Dec, Volume: 271, Issue:3
The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.
AID1346159Human alpha2C-adrenoceptor (Adrenoceptors)1994The Journal of pharmacology and experimental therapeutics, Dec, Volume: 271, Issue:3
The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.
AID1346049Human alpha2A-adrenoceptor (Adrenoceptors)1989European journal of pharmacology, Sep-22, Volume: 168, Issue:3
Novel alpha 2-adrenoceptor antagonists show selectivity for alpha 2A- and alpha 2B-adrenoceptor subtypes.
AID274936Antagonist effect on compound A-induced antinociception in Swiss Albino mouse at 1 mg/kg, ip2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Arylpiperazinylalkylpyridazinones and analogues as potent and orally active antinociceptive agents: synthesis and studies on mechanism of action.
AID274933Antinociceptive activity in Swiss Albino mouse at 1 mg/kg, ip by abdominal constriction assay2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Arylpiperazinylalkylpyridazinones and analogues as potent and orally active antinociceptive agents: synthesis and studies on mechanism of action.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (82)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (1.22)18.7374
1990's21 (25.61)18.2507
2000's39 (47.56)29.6817
2010's19 (23.17)24.3611
2020's2 (2.44)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 (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other82 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research Highlights

Pharmacokinetics (1)

ArticleYear
Spatiotemporal interaction of alpha(2) autoreceptors and noradrenaline transporters in the rat locus coeruleus: implications for volume transmission.
Journal of neurochemistry, Volume: 74, Issue: 6
2000
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioavailability (1)

ArticleYear
Role of alpha 2-adrenoceptors in the regulation of intestinal water transport.
British journal of pharmacology, Volume: 120, Issue: 5
1997
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (1)

ArticleYear
Preclinical characterization of BRL 44408: antidepressant- and analgesic-like activity through selective alpha2A-adrenoceptor antagonism.
The international journal of neuropsychopharmacology, Volume: 13, Issue: 9
2010
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]