Tezampanel

Tezampanel (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name) (developmental code names LY-293,558, LY-326,325, NGX-424) is a drug originally developed by Eli Lilly^[1] which acts as a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family,^[2][3] with selectivity for the GluR5 subtype of the kainate receptor.^[4][5] It has neuroprotective^[6] and anticonvulsant properties,^[7] the former of which may, at least in part, occur via blockade of calcium uptake into neurons.^[8]

Tezampanel

Clinical data
Other names	LY-293,558; LY-293558; LY293558; LY-326,325; LY-326325; LY326325; NGX-424; NGX424
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	154652-83-2 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	279.344 g·mol−1
3D model (JSmol)	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?)  (verify)

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,^[9][10][11] and the development of tolerance,^[12] as well as having antihyperalgesic^[13] and analgesic effects in its own right.^{[14][15][16][17][18]} It also has anxiolytic effects in animal studies and has been suggested as a candidate for the treatment of anxiety in humans.^[19]

Whereas tezampanel free base is known as LY-293558, tezampanel hydrochloride is said to be known as LY-326325.^[20][21]