Adenosine receptor inhibitor 1

Modify Date: 2024-01-19 12:23:42

Adenosine receptor inhibitor 1 Structure
Adenosine receptor inhibitor 1 structure
Common Name Adenosine receptor inhibitor 1
CAS Number 2550400-52-5 Molecular Weight 395.82
Density N/A Boiling Point N/A
Molecular Formula C17H19ClFN5O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Adenosine receptor inhibitor 1


Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases[1].

 Names

Name Adenosine receptor inhibitor 1

 Adenosine receptor inhibitor 1 Biological Activity

Description Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases[1].
Related Catalog
Target

A1AR:>1000 nM (Ki)

A2AR:68.5 nM (Ki)

hA2B:>1000 nM (Ki)

Adenosine A3 receptor:>1000 nM (Ki)

In Vitro Adenosine receptor inhibitor 1 (compound 12d) (120 min) shows metabolic stability incubated with with 96.56 and 97.97% of the parent compound remained in the reaction mixtures after incubation with mouse (MLMs) and rat liver microsomes (RLMs), respectively[1].
In Vivo Adenosine receptor inhibitor 1 (20, 30, 40 mg/kg; i.p.) shows antinociceptive activity at a concentration-dependent mannner[1]. Adenosine receptor inhibitor 1 (20 mg/kg; i.p.) shows anti-inflammatory effect in carrageenan-induced edema model[1]. Adenosine receptor inhibitor 1 (5, 10, 20 mg/kg; i.p.) shows analgesic effect in mouse[1]. Animal Model: 18-26 g male albino Swiss mice (chronic pain induced by the administration of 5% formalin) [1] Dosage: 20, 30, 40 mg/kg Administration: I.p. Result: Showed antinociceptive activity with decreasesed the licking/biting time of the right hind paw of mice in response to the irritating chemical stimulus. Animal Model: 150-180 g male rats Wistar(carrageenan-induced edema model)[1] Dosage: 20 mg/kg Administration: I.p. Result: Showed anti-inflammatory effect with the inhibition of 23.3%, 54.2%, 66.0% at 1h, 2h, 3h, respectively. Animal Model: Mouse (induce pain of peripheral origin by injection of an irritant like phenylbenzoquinone or acetic acid in mice)[1] Dosage: 5, 10, 20 mg/kg Administration: I.p. Result: Showed peripheral analgesic effect with the significant decrease in the number of writhings by 32.9%, 54.9%, 82.0% at doses of 5, 10, 20 mg/kg, respectively.
References

[1]. Załuski M, et al. 8-Benzylaminoxanthine scaffold variations for selective ligands acting on adenosine A2A receptors. Design, synthesis and biological evaluation. Bioorg Chem. 2020 Aug;101:104033.

 Chemical & Physical Properties

Molecular Formula C17H19ClFN5O3
Molecular Weight 395.82
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.
Top Suppliers:I want be here
Related Compounds: More...
Adenosine receptor inhibitor 2
2550401-76-6
Edg-2 receptor inhibitor 1
1195941-38-8
CCK-A receptor inhibitor 1
137004-80-9
Adenosine receptor antagonist 1
2682930-40-9
Adenosine receptor antagonist 3
2400864-80-2
Adenosine receptor antagonist 2
2703054-47-9
Adenosine-1′-13C
201996-55-6
9-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-[[2-(trifluoromethyl)phenyl]methylamino]-1H-purin-2-one
62190-55-0
Adenosine, 1-methyl-,hydriodide (1:1)
34308-25-3
5-chloro-N-(2-(4-cyclopropyl-5-oxo-3-(thiophen-2-yl)-4,5-dihydro-1H-1,2,4-triazol-1-yl)ethyl)thiophene-2-carboxamide
1448077-74-4
6-Methyl-3-(trifluoromethyl)-2H-chromen-2-one
1562426-71-4
N-{2-[4-cyclopropyl-5-oxo-3-(thiophen-2-yl)-4,5-dihydro-1H-1,2,4-triazol-1-yl]ethyl}-1-methyl-1H-1,2,3-triazole-4-carboxamide
1448046-53-4
N-(2-(4-cyclopropyl-5-oxo-3-(thiophen-2-yl)-4,5-dihydro-1H-1,2,4-triazol-1-yl)ethyl)-2-(3,5-dimethylisoxazol-4-yl)acetamide
1448027-96-0
N-(2-(4-cyclopropyl-5-oxo-3-(thiophen-2-yl)-4,5-dihydro-1H-1,2,4-triazol-1-yl)ethyl)-1H-indole-6-carboxamide
1448131-97-2
N-(2-(4-cyclopropyl-5-oxo-3-(thiophen-2-yl)-4,5-dihydro-1H-1,2,4-triazol-1-yl)ethyl)cyclohex-3-enecarboxamide
1448130-37-7
N-(2-(4-cyclopropyl-5-oxo-3-(thiophen-2-yl)-4,5-dihydro-1H-1,2,4-triazol-1-yl)ethyl)-4-(trifluoromethoxy)benzamide
1448125-59-4
N-(2-(4-cyclopropyl-5-oxo-3-(thiophen-2-yl)-4,5-dihydro-1H-1,2,4-triazol-1-yl)ethyl)-2-(4,5-dimethyl-6-oxopyrimidin-1(6H)-yl)acetamide
1448034-54-5
N-(2-(4-cyclopropyl-5-oxo-3-(thiophen-2-yl)-4,5-dihydro-1H-1,2,4-triazol-1-yl)ethyl)-5-(thiophen-2-yl)isoxazole-3-carboxamide
1448053-41-5
5-(5-bromothiophen-2-yl)-N-[2-(1H-imidazol-5-yl)ethyl]pyrazolidine-3-carboxamide
1491130-80-3