GR 79236 Property

Boiling point:

728.3±70.0 °C(Predicted)

Density 

1.89±0.1 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

H₂O: 12 mg/mL

form 

solid

pka

13.12±0.70(Predicted)

color 

white

Safety

Hazard Codes 

Xn

Risk Statements 

22-36/37/38

Safety Statements 

26-36

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

GR 79236 Chemical Properties,Usage,Production

Uses

GR 79236 is an Adenosine A1-R agonist.

Definition

ChEBI: (2R,3R,4S,5R)-2-[6-[[(1S,2S)-2-hydroxycyclopentyl]amino]-9-purinyl]-5-(hydroxymethyl)oxolane-3,4-diol is a purine nucleoside.

Biological Activity

Adenosine A 1 receptor agonist (K i = 3.1 nM). Anticonvulsive in mice following systemic administration in vivo .

in vitro

gr79236 is a highly potent and selective a1 receptor agonist which is originally developed for the treatment of type 2 diabetes mellitus, as a cardioprotective agent and also for peripheral arterial occlusive diseases. gr79236 inhibited catecholamine-induced lipolysis in adipocytes at low concentrations [1]

in vivo

gr79236 has a pronounced effect on nefa and tg levels in both acute and chronic animal models, thus establishing the potential of this approach for the treatment of t2d [1]. gr79236 also can inhibit neurogenic vasodilation in anaesthetized rats, inhibit electrical stimulation of superior saggital sinusinduced trigeminovascular nociceptive transmission and cgrp release in anaesthetized cats and inhibit trigeminal nociception in humans [2].

IC 50

3.1 nm (ki)

References

[1] kiesman wf, elzein e, zablocki j. a1 adenosine receptor antagonists, agonists, and allosteric enhancers. handb exp pharmacol. 2009;(193):25-58.
[2] arulmani u, heiligers jp, centurión d, garrelds im, villalón cm, saxena pr. 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.
[3] sneyd jr, langton ja, allan lg, peacock je, rowbotham dj. multicentre evaluation of the adenosine agonist gr79236x in patients with dental pain after third molar extraction. br j anaesth. 2007 may;98(5):672-6. epub 2007 apr 7.