166974-23-8

166974-23-8 structure
166974-23-8 structure
  • Name: GV-196771A
  • Chemical Name: sodium,4,6-dichloro-3-[(2-oxo-1-phenylpyrrolidin-3-ylidene)methyl]-1H-indole-2-carboxylate
  • CAS Number: 166974-23-8
  • Molecular Formula: C20H13Cl2N2NaO3
  • Molecular Weight: 423.22500
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
  • Create Date: 2016-10-02 01:47:39
  • Modify Date: 2024-01-28 13:08:40
  • GV-196771A is the sodium salt form of GV196771, is an NMDA receptor antagonist.

Name sodium,4,6-dichloro-3-[(2-oxo-1-phenylpyrrolidin-3-ylidene)methyl]-1H-indole-2-carboxylate
Synonyms GV-196771A
Description GV-196771A is the sodium salt form of GV196771, is an NMDA receptor antagonist.
Related Catalog
Target

NMDA receptor[1]

In Vivo GV196771 is a potent antagonist of the modulatory glycine site of the N-methyl-D-aspartate receptor. GV196771 is a potent antagonist of the modulatory glycine site of the NMDA receptor developed for treatment of neuropathic pain. GV196771 is an NMDA receptor antagonist with low oral bioavailability in rats and mice. GV196771 has low oral bioavailability (<10%) and plasma clearance (~2 mL/min/kg) in rats[1].
Animal Admin Mice[1] Male wild-type FVB mdr1a/1b+/+ and Pgp-deficient knockout FVBmdr1a/1b-/- mice (20-30 g) are used. Dose solutions of 0.2 mg/mL for GV196771 and 5.0 mg/mL for GF120918 are prepared fresh using 0.5% hydroxypropylmethylcellulose and 1% Tween 80 as a vehicle. Two hours before the administration of GV196771, the animals are divided into two groups. One group receive a single oral dose (10 mL/kg) of vehicle and the second group receive a single 50 mg/kg oral dose (10 mL/kg) of GF120918. Two hours later, all animals receive a single 2 mg/kg oral dose (10 mL/kg) of GV196771. At scheduled time points, mice are anesthetized with CO2 and blood samples are obtained by cardiac puncture. Blood is centrifuged to yield plasma. The MDR genotype of each animal is confirmed by a polymerase chain reaction assay after study completion.
References

[1]. Polli JW, et al. The systemic exposure of an N-methyl-D-aspartate receptor antagonist is limited in mice by the P-glycoprotein and breast cancer resistance protein efflux transporters. Drug Metab Dispos. 2004 Jul;32(7):722-6.

Boiling Point 644.9ºC at 760mmHg
Molecular Formula C20H13Cl2N2NaO3
Molecular Weight 423.22500
Flash Point 343.8ºC
Exact Mass 422.02000
PSA 76.23000
LogP 3.72350
Vapour Pressure 1.64E-17mmHg at 25°C
Storage condition 2-8℃