| Description | SIB-1757 (6-methyl-2-[(E)-phenyldiazenyl]pyridin-3) is a selective antagonist of mGlu5 metabotropic glutamate receptor subtype (hmGlu5, IC50 : 0.4 μM) |
| In vivo | SIB-1757 was given by either intrathecal (i.th.), subcutaneous (s.c.) or intraplantar (i.pl.) injection.?In SNL rats, i.th.?SIB-1757 produced a partial reversal of tactile allodynia with a shallow dose-response curve ranging over three-orders of magnitude;?SIB-1757 was inactive against allodynia when given systemically.?SIB-1757 produced full reversal of thermal hyperalgesia in SNL rats following administration either spinally or locally to the injured paw;?administration to the contralateral paw had no effect.?SIB-1757 did not produce antinociception in either the SNL or sham-operated rats by any route[1]. |
| Target activity | mGlu5 (human):0.4 μM |
| Synonyms | 6-methyl-2-[(E)-phenyldiazenyl]pyridin-3 |
| molecular weight | 213.24 |
| Molecular formula | C12H11N3O |
| CAS | 31993-01-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 5.5 mg/mL (25.79 mM), Sonication is recommended. |
| References | 1. Dogrul A , Ossipov M H , Lai J , et al. Peripheral and spinal antihyperalgesic activity of SIB-1757, a metabotropic glutamate receptor (mGLUR5) antagonist, in experimental neuropathic pain in rats[J]. 2000, 292(2):0-118. 2. Varney M A A , Cosford N D P , Jachec C , et al. SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5[J]. Journal of Pharmacology & Experimental Therapeutics, 1999, 290(1):170-181. |