Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C15H21N5O5 |
| Molecular Weight | 351.3577 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 6 / 6 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC[C@H]1O[C@H]([C@H](O)[C@@H]1O)N2C=NC3=C2N=CN=C3N[C@H]4CCC[C@@H]4O
InChI
InChIKey=GYWXTRVEUURNEW-TVDBPQCTSA-N
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
| Molecular Formula | C15H21N5O5 |
| Molecular Weight | 351.3577 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 6 / 6 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
GR79236 is an adenosine A1 receptor agonist, which possesses cardiovascular and antilipolytic properties. GR79236 was studied in model animals for the treatment of diabetic ketoacidosis and in patients for pain relief. However, these studies were discontinued. In addition, analgesic efficacy of GR79236 was investigated in the dental pain model. Nevertheless, there was no evidence of efficacy of GR79236. A higher dose of GR79236 might have been effective or that was suggested, that intravenous administration of that drug did not achieve appropriate concentrations in the brain or peripheral nerves.
Originator
Approval Year
Sample Use Guides
Seventy-nine patients with moderate pain after third molar extraction under general anaesthesia were randomized to receive a 15 min double-blind infusion containing either GR79236X 4 microg kg-1, GR79236X 10 microg kg-1, diclofenac 50 mg, or saline placebo. Rescue analgesia was promptly available to all patients.
Route of Administration:
Intravenous
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.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:33:40 UTC 2023
by
admin
on
Fri Dec 15 16:33:40 UTC 2023
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| Record UNII |
Q4H682B2VZ
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| Record Status |
Validated (UNII)
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| Record Version |
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-
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Q4H682B2VZ
Created by
admin on Fri Dec 15 16:33:40 UTC 2023 , Edited by admin on Fri Dec 15 16:33:40 UTC 2023
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DTXSID10154427
Created by
admin on Fri Dec 15 16:33:40 UTC 2023 , Edited by admin on Fri Dec 15 16:33:40 UTC 2023
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9884817
Created by
admin on Fri Dec 15 16:33:40 UTC 2023 , Edited by admin on Fri Dec 15 16:33:40 UTC 2023
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124555-18-6
Created by
admin on Fri Dec 15 16:33:40 UTC 2023 , Edited by admin on Fri Dec 15 16:33:40 UTC 2023
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| Related Record | Type | Details | ||
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TARGET -> AGONIST |
Rat brain receptor
BINDING
Ki
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OFF TARGET->WEAK AGONIST |
Rat brain receptor
BINDING
Ki
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
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