GR 79236 - CAS 124555-18-6
Catalog number: 124555-18-6
Category: Inhibitor
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Molecular Formula:
C15H21N5O5
Molecular Weight:
351.36
COA:
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Targets:
Adenosine Receptor
Description:
GR 79236, an effective Adenosine A1 receptor agonist, could probably be used as an anti-inflammatory agent. IC50: 3.1 nM(Ki).
Purity:
95%
Appearance:
White solid
Synonyms:
GR79236; GR-79236; GR 79236. N-[(1S, trans)-2-Hydroxycyclopentyl]adenosine
Solubility:
100 mM in H2O
Storage:
-20ºC Freeze
MSDS:
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Application:
GR 79236 is an effective Adenosine A1 receptor agonist that could probably be used as an anti-inflammatory agent.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
Boiling Point:
728.3ºC at 760mmHg
Density:
1.89g/cm3
InChIKey:
GYWXTRVEUURNEW-QPIWWKSXSA-N
InChI:
InChI=1S/C15H21N5O5/c21-4-9-11(23)12(24)15(25-9)20-6-18-10-13(16-5-17-14(10)20)19-7-2-1-3-8(7)22/h5-9,11-12,15,21-24H,1-4H2,(H,16,17,19)/t7-,8-,9+,11?,12-,15+/m0/s1
Canonical SMILES:
C1CC(C(C1)O)NC2=NC=NC3=C2N=CN3C4C(C(C(O4)CO)O)O
1.Functional characterization of three adenosine receptor types.
Gurden MF;Coates J;Ellis F;Evans B;Foster M;Hornby E;Kennedy I;Martin DP;Strong P;Vardey CJ Br J Pharmacol. 1993 Jul;109(3):693-8.
1. The purpose of the present study was to classify adenosine receptors into A1 and A2 subtypes in a wide range of isolated tissues and cell types (rat adipocytes and atria, guinea-pig ileum and atria (A1); guinea-pig aorta, dog coronary artery and human platelets and neutrophils (A2)) using the R- and S-diastereoisomers of N-phenylisopropyladenosine (PIA), N-cyclopentyladenosine (CPA), the novel compound, N-[(1S,trans)-2-hydroxycyclopentyl]adenosine (GR79236), N-[(2-methylphenyl)methyl]adenosine (metrifudil), 2-(phenylamino)adenosine (CV1808), and 2[[2-[4-(2-carboxyethyl)phenyl]ethyl]amino]-N- ethylcarboxamidoadenosine (CGS21680); N-ethylcarboxamidoadenosine (NECA) was used as a standard. 2. Results obtained in all tissue preparations previously reported to contain A1-receptors could be described by a single rank order of agonist potency: CPA > or = GR79236, R-PIA > or = NECA >> S-PAI > or = metrifudil > or = CV1808, CGS21680. 3. In contrast, two distinct rank orders of agonist potency were observed in preparations previously reported to contain A2-receptors. In dog coronary artery, human neutrophils and platelets the rank order of potency was: CV1808, CGS21680 > or = NECA > R-PIA > or = metrifudil > or = CPA > GR79236 S-PIA.
2.In vitro effect of adenosine agonist GR79236 on the insulin sensitivity of glucose utilisation in rat soleus and human rectus abdominus muscle.
Webster JM;Heseltine L;Taylor R Biochim Biophys Acta. 1996 Jun 7;1316(2):109-13.
The dose-response effects of a new adenosine agonist, GR79236, were examined in isolated rat soleus muscle strips and human rectus abdominus muscle strips. Effects on the insulin sensitivity of carbohydrate metabolism were examined, in particular upon insulin stimulated glycogen synthesis and glycolytic flux. In the presence of adenosine deaminase (ADA), GR79236 increased insulin sensitivity of pyruvate release from rat soleus muscle strips by 24% from 82.5 +/- 10.0 to 102.5 +/- 10.0 (P < 0.01), by 27% to 105.0 +/- 12.5 (P < 0.01) and by 24% to 102.5 +/- 10.0 (P < 0.01) nmol/25 mg per h at 0.1 and 10 microM GR79236, respectively. Rates of lactate release followed a similar but non-significant trend. Addition of GR79236 in the presence of ADA had no effect on rates of glycogen synthesis. Insulin stimulated rates of pyruvate or lactate release or of glycogen synthesis were unaffected by the addition of adenosine deaminase or GR79236 in human rectus abdominus muscle strips. Adenosine agonists may act indirectly to modulate insulin sensitivity of carbohydrate metabolism.
3.Adenosine A1 receptor-mediated excitation of nociceptive afferents innervating the normal and arthritic rat knee joint.
Dowd E;McQueen DS;Chessell IP;Humphrey PP Br J Pharmacol. 1998 Nov;125(6):1267-71.
We tested the hypothesis that adenosine excites nociceptive primary afferents innervating the knee joint. Neuronal recordings were made from fine nerve filaments innervating the knee joint in rats anaesthetized with pentobarbitone. Drugs were injected close-arterially (i.a.) or into the articular space (i.art.). We studied normal and chronically inflamed arthritic joints, the latter 14-21 days after a single intra-articular injection of Freund's Complete Adjuvant, performed under halothane anaesthesia. Adenosine injected i.a. caused delayed (approximately 10 s) excitation of the majority of polymodal C-fibre afferents, and had similar effects when injected directly into the joint. Adenosine triphosphate (ATP) had biphasic effects on discharge, a fast (<1 s) excitation was followed by a delayed increase similar to that seen with adenosine. The adenosine A1 receptor agonists N6-cyclopentyladenosine (CPA) and N-[(1S,trans)-2-hydroxypentyl] adenosine (GR79236) also excited the C-fibre afferents. The A1 antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) antagonized the responses evoked by adenosine, CPA, and the delayed increase seen after ATP, indicating that excitation of the nociceptive afferents was mediated via adenosine A1 receptors.
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Chemical Structure

CAS 124555-18-6 GR 79236

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