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EMA401 sodium

Names

[ CAS No. ]:
1316755-17-5

[ Name ]:
EMA401 sodium

[Synonym ]:
3-Isoquinolinecarboxylic acid, 2-(2,2-diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-, sodium salt, (3S)- (1:1)
Sodium (3S)-5-(benzyloxy)-2-(diphenylacetyl)-6-methoxy-1,2,3,4-tetrahydro-3-isoquinolinecarboxylate
MFCD30502664

Biological Activity

[Description]:

Olodanrigan (EMA401) sodium is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. Olodanrigan sodium is under development as a neuropathic pain therapeutic agent. Olodanrigan sodium analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons[1][2][3][4].

[Related Catalog]:

Research Areas >> Endocrinology
Signaling Pathways >> GPCR/G Protein >> Angiotensin Receptor
Research Areas >> Neurological Disease

[Target]

"Reverse Transcriptase[1] HIV[1]"


[In Vivo]

EMA401 sodium（10mg/kg；口服）导致慢性压迫性损伤 (CCI) 后第 14 天大鼠的 θ 功率显着减弱和缩爪潜伏期 (PWL) 增加[4]。

[References]

[1]. Rice AS et al. EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomised, double-blind, placebo-controlled phase 2 clinical trial.Lancet. 2014 May 10;383(9929):1637-47.  

[2]. Anand U et al. Mechanisms underlying clinical efficacy of Angiotensin II type 2 receptor (AT2R) antagonist EMA401 in neuropathic pain: clinical tissue and in vitro studies. Mol Pain. 2015 Jun 26;11:38.  

[3]. Suguru Koyama,et al. An Electroencephalography Bioassay for Preclinical Testing of Analgesic Efficacy.

Chemical & Physical Properties

[ Molecular Formula ]:
C32H28NNaO5

[ Molecular Weight ]:
529.56

[ Exact Mass ]:
529.186523

Related Compounds