Page last updated: 2024-12-07

(3,4-dihydroxyphenylamino)-2-imidazoline

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

Description

(3,4-dihydroxyphenylamino)-2-imidazoline is a chemical compound, also known as **CL 218,872**. It's a selective **α2-adrenoceptor agonist**, which means it activates a specific type of receptor in the body.

**Why it's important for research:**

* **Potential therapeutic applications:** CL 218,872 has shown promising results in preclinical studies for a variety of conditions, including:
* **Hypertension:** It can lower blood pressure by activating α2-adrenoceptors in the central nervous system, leading to a decrease in sympathetic outflow.
* **Pain management:** It can reduce pain by inhibiting the release of neurotransmitters involved in pain perception.
* **Anxiety and depression:** Its action on α2-adrenoceptors may have antidepressant and anxiolytic effects.
* **Neuroprotection:** It may have neuroprotective properties, potentially protecting neurons from damage.
* **Understanding α2-adrenoceptor function:** CL 218,872 is a valuable research tool for studying the role of α2-adrenoceptors in various physiological processes. It allows researchers to investigate the effects of activating these receptors in different tissues and organs.
* **Drug development:** CL 218,872 serves as a lead compound for the development of new drugs targeting α2-adrenoceptors. By modifying its structure, researchers aim to enhance its potency, selectivity, and pharmacokinetic properties for improved therapeutic outcomes.

**It is important to note that CL 218,872 is not currently approved for clinical use. Further research is needed to determine its safety and efficacy in humans.**

**Other important points:**

* CL 218,872 is closely related to **guanfacine** and **clonidine**, which are α2-adrenoceptor agonists already approved for clinical use.
* It exhibits a high affinity for α2A-adrenoceptors, making it a valuable tool for studying the specific role of this receptor subtype.

Overall, (3,4-dihydroxyphenylamino)-2-imidazoline (CL 218,872) is a promising compound with potential therapeutic applications in various fields. However, further research is necessary to fully understand its safety and efficacy in humans.

(3,4-dihydroxyphenylamino)-2-imidazoline: potent agonist at dopamine receptors mediating neuronal inhibition; RN given refers to parent cpd; structure in UD indicates phenyl-imino group [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID123703
CHEMBL ID146100
SCHEMBL ID9421173
SCHEMBL ID5429353
MeSH IDM0058334

Synonyms (14)

Synonym
2-(3,4-dihydroxyphenylimino)imidazolidine
(3,4-dihydroxyphenylamino)-2-imidazoline
1,2-benzenediol, 4-((4,5-dihydro-1h-imidazol-2-yl)amino)-
CHEMBL146100 ,
57101-49-2
SCHEMBL9421173
dea5vw1n6r ,
unii-dea5vw1n6r
SCHEMBL5429353
2-(3,4-dihydroxyphenylimino)-imidazolidine
bdbm50225294
4-[(4,5-dihydro-1h-imidazol-2-yl)amino]benzene-1,2-diol
DTXSID40972570
Q27276347

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Moreover, we examined a potential renal toxic mechanism(s) of arsenic trioxide by using a toxicity-related gene and investigated potential treatments to reduce the renal toxicity of arsenic trioxide."( An approach to elucidate potential mechanism of renal toxicity of arsenic trioxide.
Fujimura, A; Oshima, Y; Sasaki, A, 2007
)
0.34
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (3)

Assay IDTitleYearJournalArticle
AID36795Binding affinity against alpha-2 adrenergic receptor is the ability to inhibit the specific [3H]clonidine binding (0.4 nM) to rat isolated brain membranes by 50% was reported.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID197169Hypertensive activity (increase in arterial pressure to 60 mmHg)) after i.v. administration to pithed rats.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
AID36715Binding affinity against alpha-1 adrenergic receptor is the ability to inhibit the specific [3H]prazosin binding (0.4 nM) to rat isolated brain membranes by 50% was reported.1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (64)

TimeframeStudies, This Drug (%)All Drugs %
pre-199021 (32.81)18.7374
1990's14 (21.88)18.2507
2000's25 (39.06)29.6817
2010's3 (4.69)24.3611
2020's1 (1.56)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.16

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 Index10.16 (24.57)
Research Supply Index4.17 (2.92)
Research Growth Index4.33 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.16)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (1.56%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other63 (98.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]