GR 79236

Names

[ Name ]:
GR 79236

[Synonym ]:
HMS3268O08
N-[(1S (trans)-2-Hydroxycyclopentyl]adenosine
GR79236

Biological Activity

[Description]:

GR79236 is a highly potent and selective adenosine A1 receptor agonist (Ki = 3.1 nM) that has analgesic and anti-inflammatory actions in humans and animals.IC50 value: 3.1 nM(Ki)Target: adenosine A1 receptorin vitro: GR79236 is a highly potent and selective A1-receptor agonist that is originally developed for the treatment of Type 2 diabetes mellitus, as a cardioprotective agent and also for peripheral arterial occlusive diseases.in vivo: GR79236 has also been shown to have antinociceptive and anti-inflammatory properties in animal models. GR79236 inhibits the release of CGRP evoked by superior sagittal sinus (SSS) stimulation in the cat and inhibits trigeminal nucleus firing in the cat and rat. GR79236X has acute, short-term analgesic efficacy.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

Research Areas >> Inflammation/Immunology

[References]

[1]. Sneyd JR, et al. Multicentre evaluation of the adenosine agonist GR79236X in patients with dental pain after third molar extraction. Br J Anaesth. 2007 May;98(5):672-676.

[2]. Arulmani U, et al. Lack of effect of the adenosine A1 receptor agonist, GR79236, on capsaicin-induced CGRP release in anaesthetized pigs. Cephalalgia. 2005 Nov;25(11):1082-90.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.89g/cm3

[ Boiling Point ]:
728.3ºC at 760mmHg

[ Molecular Formula ]:
C₁₅H₂₁N₅O₅

[ Molecular Weight ]:
351.35800

[ Flash Point ]:
394.3ºC

[ Exact Mass ]:
351.15400

[ PSA ]:
145.78000

[ Vapour Pressure ]:
0mmHg at 25°C

[ Index of Refraction ]:
1.846

[ Storage condition ]:
2-8℃

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
R22

[ Safety Phrases ]:
26-36

[ RIDADR ]:
NONH for all modes of transport

Articles

Multicentre evaluation of the adenosine agonist GR79236X in patients with dental pain after third molar extraction.

Br. J. Anaesth. 98(5) , 672-6, (2007)

Adenosine is analgesic in humans, and the selective adenosine A1 receptor agonist GR79236X has significant anti-nociceptive activity in an animal pain model of inflammatory pain.Seventy-nine patients ...

Does a selective adenosine A(1) receptor agonist protect against exercise induced ischaemia in patients with coronary artery disease?

Heart 87(2) , 115-20, (2002)

The "warm up" effect in angina may represent ischaemic preconditioning, which is mediated by adenosine A(1) receptors in most models.To investigate the effect of a selective A(1) agonist, GR79236 (Gla...

Improvement of ketoacidosis in the diabetic rat after the administration of the oral antilipolytic agent GR 79236.

Clin. Sci. 86(5) , 593-8, (1994)

1. We assessed the effect of a novel oral antilipolytic agent, N-[(1S, trans)-2-hydroxycyclopentyl]adenosine (GR 79236), in experimental diabetic ketoacidosis. Ketotic rats were gavaged with GR 79236 ...

Related Compounds

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