SIB-1757 是高选择性非竞争性mGlu5 受体拮抗剂 (IC50:0.4 μM) 。

SIB-1757 is a selective antagonist of mGlu5 metabotropic glutamate receptor subtype (hmGlu5, IC50 : 0.4 μM)

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].

31993-01-8

C12H11N3O

213.24

6-methyl-2-[(E)-phenyldiazenyl]pyridin-3

DMSO:17 mg/ml(79.72 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years