| CAS NO: | 186141-75-3 |
| 规格: | ≥98% |
| Molecular Weight (MW) | 375.17 |
|---|---|
| Formula | C11H14IN5O2 |
| CAS No. | 186141-75-3 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 10 mM |
| Water: N/A | |
| Ethanol: N/A | |
| Other info | Chemical Name: (1S,2R,3S,5R)-3-amino-5-{4-amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl}cyclopentane-1,2-diol InChi Key: NSXJHIFQIZKLGF-LWIVVEGESA-N InChi Code: InChI=1S/C11H14IN5O2/c12-4-2-17(6-1-5(13)8(18)9(6)19)11-7(4)10(14)15-3-16-11/h2-3,5-6,8-9,18-19H,1,13H2,(H2,14,15,16)/t5-,6+,8+,9-/m0/s1 SMILES Code: O[C@@H]1[C@H](O)[C@@H](N)C[C@H]1N2C=C(I)C3=C(N)N=CN=C32 |
| Synonyms | A134974; A 134974; A-134974 |
| In Vitro | In vitro activity: AK enzyme inhibition was assayed radiochemically as described byYamada et al. (1980) and McNally et al. (1997). The ability of A-134974 to inhibit AK activity in intact IMR-32 neuroblastoma cells (American Type Culture Collection, Gaithersburg, MD) carried out as previously described (Kowaluk and Cowart, 1994). Radioligand binding assay methodology for the A1, A2A, and A3 receptors was carried out as described by Jarvis et al. (2000). The ability of A-134974 to inhibit [3H]nitrobenzylthioinosine binding to the ADO transporter and to inhibit adenosine deaminase activity was also examined using previously described methodology (Parkinson and Geiger, 1996). |
|---|---|
| In Vivo | Drugs administered to rats were A-134974 (Cowart, 1997, an AK inhibitor synthesized at Abbott Laboratories), morphine sulfate (Mallinckrodt, St. Louis, MO), and theophylline (a nonselective ADO receptor antagonist; Sigma Chemical Co., St. Louis, MO). All drugs were dissolved in sterile water for local (intraplantar, i.t., or i.c.v.) or systemic (i.p.) delivery. The drug administration procedures described below were followed for locomotor activity experiments as well as for hyperalgesia experiments. Each experimental group consisted of at least five animals. |
| Animal model | Male Sprague-Dawley rats (260–320 g) |
| Formulation & Dosage | Systemic Administration of A-134974: A-134974 (0.3–30 μmol/kg) or vehicle was administered i.p. 30 min before testing. Local Administration of A-134974: A-134974 (3–100 nmol) or vehicle was injected directly into 1) the lumbar spinal cord via indwelling intrathecal catheters, 2) the right lateral ventricle, or 3) the intraplantar region of a carrageenan-inflamed hindpaw (hyperalgesia experiments only). |
| References | J Pharmacol Exp Ther. 2001 Feb;296(2):501-9. |
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