GR 79236

Modify Date: 2024-01-08 11:48:36

GR 79236 Structure
GR 79236 structure
Common Name GR 79236
CAS Number 124555-18-6 Molecular Weight 351.35800
Density 1.89g/cm3 Boiling Point 728.3ºC at 760mmHg
Molecular Formula C15H21N5O5 Melting Point N/A
MSDS Chinese USA Flash Point 394.3ºC
Symbol GHS07
GHS07
Signal Word Warning

 Use of GR 79236


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.

 Names

Name (2R,3R,4S,5R)-2-[6-[[(1S,2S)-2-hydroxycyclopentyl]amino]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol
Synonym More Synonyms

 GR 79236 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
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.

 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
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

 Articles26

More 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 ...

 Synonyms

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