Eglumegad

Eglumegad

Clinical data
ATC code	none
Identifiers
IUPAC name (1S,2S,5R,6S)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid
CAS Number	176199-48-7 Y
PubChem CID	213056
IUPHAR/BPS	1393
ChemSpider	184747 N
UNII	ONU5A67T2S
Chemical and physical data
Formula	C8H11NO4
Molar mass	185.18 g/mol
3D model (Jmol)	Interactive image
SMILES O=C(O)[C@H]1[C@]2([H])CC[C@](C(O)=O)(N)[C@@]21[H]
InChI InChI=1S/C8H11NO4/c9-8(7(12)13)2-1-3-4(5(3)8)6(10)11/h3-5H,1-2,9H2,(H,10,11)(H,12,13)/t3-,4-,5-,8-/m0/s1 N Key:VTAARTQTOOYTES-RGDLXGNYSA-N N
NY (what is this?)

Eglumegad (LY354740) is a research drug developed by Eli Lilly and Company, which is being investigated for its potential in the treatment of anxiety and drug addiction. It is a glutamate derived compound and its mode of action implies a novel mechanism.

Eglumegad acts as a group-selective agonist for the group II metabotropic glutamate receptors (mGluR_2/3). It is unclear whether eglumegad directly interacts with dopamine D2 receptors.

In experiments on mice, eglumegad was found to be as effective as diazepam for treating anxiety symptoms in several standard tests, but without producing any of the negative side effects of diazepam such as sedation and memory impairment. Tests in humans confirmed that it produced anxiolytic effects without producing sedation. However it did slightly reduce cognitive performance in tests on monkeys.

Eglumegad has also been found to be effective in relieving the symptoms of withdrawal from chronic use of both nicotine and morphine in animals, as well as inhibiting the development of tolerance to morphine, raising hope that this drug may be useful for treating drug addiction in humans.

Eglumegad and related drugs are neuroprotective and are synergistic with the neuroprotection produced by N-methyl-D-aspartic acid (NMDA) antagonist drugs, which may make these drugs useful in aiding recovery from brain injury.

This class of drugs also interacts with hallucinogenic drugs, with eglumegad reducing the effects of 5HT_2A agonist hallucinogens, while conversely the mGluR_2/3 antagonist LY341495 increased the behavioural effects of these drugs. This suggests that mGluR_2/3 agonists such as eglumegad may have potential uses in the treatment of some forms of psychosis, although eglumegad had only limited effects on the action of the dissociative drug phencyclidine which is generally a better model for schizophrenia than the 5HT_2A agonist hallucinogens.