Tezampanel

Tezampanel

Clinical data
Routes of administration	IV
ATC code	none
Legal status
Legal status	Investigational
Identifiers
IUPAC name (3S,4aR,6R,8aR)-6-[2-(1H-tetrazol-5-yl)ethyl]decahydroisoquinoline-3-carboxylic acid
CAS Number	150131-78-5 Y
PubChem CID	127894
IUPHAR/BPS	4245
ChemSpider	113428 N
UNII	GA36S2O9C2
KEGG	D06656 N
ChEMBL	CHEMBL14935 N
Chemical and physical data
Formula	C13H21N5O2
Molar mass	279.338 g/mol
3D model (Jmol)	Interactive image
SMILES C1C[C@H]2CN[C@@H](C[C@H]2C[C@H]1CCC3=NNN=N3)C(=O)O
InChI InChI=1S/C13H21N5O2/c19-13(20)11-6-10-5-8(1-3-9(10)7-14-11)2-4-12-15-17-18-16-12/h8-11,14H,1-7H2,(H,19,20)(H,15,16,17,18)/t8-,9+,10-,11+/m1/s1 N Key:ZXFRFPSZAKNPQQ-YTWAJWBKSA-N N
NY (what is this?)

Tezampanel (INN, USAN) (code names LY-293,558, NGX-424) is a drug originally developed by Eli Lilly which acts as a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family, with selectivity for the GluR5 subtype of the kainate receptor. It has neuroprotective and anticonvulsant properties, the former of which may, at least in part, occur via blockade of calcium uptake into neurons.

Tezampanel has a range of effects which may be useful for medicinal purposes, as well as its applications in scientific research. It suppresses both the withdrawal symptoms from morphine and other opioids, and the development of tolerance, as well as having antihyperalgesic and analgesic effects in its own right. It also has anxiolytic effects in animal studies and has been suggested as a candidate for the treatment of anxiety in humans.