ELPETRIGINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C10H7Cl3N4
Molecular Weight	289.548
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

NC1=NC(N)=C(N=C1)C2=C(Cl)C(Cl)=CC(Cl)=C2

InChI

InChIKey=NNXUYJFHOVCRSM-UHFFFAOYSA-N

InChI=1S/C10H7Cl3N4/c11-4-1-5(8(13)6(12)2-4)9-10(15)17-7(14)3-16-9/h1-3H,(H4,14,15,17)

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Description
Sources: https://adisinsight.springer.com/drugs/800027454 | https://www.ncbi.nlm.nih.gov/pubmed/19038245 | https://www.ncbi.nlm.nih.gov/pubmed/18377968

Elpetrigine (GW293273 or JZP-4) is potent calcium and sodium channel blocker. In animal models, elpetrigine exerts anxiolytic, anticonvulsant, antidepressant and antimania effects. Jazz Pharmaceuticals is developing elpetrigine for the treatment of mood disorders and epilepsy.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Sodium channel protein type II alpha subunit 27 Target ID: CHEMBL4187 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20502724 \| https://www.ncbi.nlm.nih.gov/pubmed/18377968 \| https://www.ncbi.nlm.nih.gov/pubmed/19008076	Blocker 555
Sodium channel protein type III alpha subunit 18 Target ID: CHEMBL5163 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20502724 \| https://www.ncbi.nlm.nih.gov/pubmed/18377968 \| https://www.ncbi.nlm.nih.gov/pubmed/19008076	Blocker 555
Voltage-gated L-type calcium channel 95 Target ID: CHEMBL2095229 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20502724 \| https://www.ncbi.nlm.nih.gov/pubmed/18377968 \| https://www.ncbi.nlm.nih.gov/pubmed/19008076	Blocker 555
Voltage-gated N-type calcium channel alpha-1B subunit 14 Target ID: CHEMBL4478 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20502724 \| https://www.ncbi.nlm.nih.gov/pubmed/18377968 \| https://www.ncbi.nlm.nih.gov/pubmed/19008076	Blocker 555
Voltage-gated P/Q-type calcium channel alpha-1A subunit 1 Target ID: CHEMBL4266 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20502724 \| https://www.ncbi.nlm.nih.gov/pubmed/18377968 \| https://www.ncbi.nlm.nih.gov/pubmed/19008076	Blocker 555

PubMed

Title	Date	PubMed
Anxiolytic effects of lamotrigine and JZP-4 in the elevated plus maze and in the four plate conflict test.	2009-01-14	19038245
In vivo pharmacological effects of JZP-4, a novel anticonvulsant, in models for anticonvulsant, antimania and antidepressant activity.	2008-06	18377968
Modifications of antiepileptic drugs for improved tolerability and efficacy.	2008-02-14	19787095

Patents

Name

Type

Language

JZP-4

Preferred Name

English

ELPETRIGINE

Official Name

English

Elpetrigine [WHO-DD]

Common Name

English

elpetrigine [INN]

Common Name

English

3-(2,3,5-Trichlorophenyl)pyrazine-2,6-diamine

Systematic Name

English

2,6-PYRAZINEDIAMINE, 3-(2,3,5-TRICHLOROPHENYL)-

Systematic Name

English

ELPETRIGINE [USAN]

Common Name

English

Code System Code Type Description

FDA UNII

1X64S9H3ZS