MFZ10-7

Details

Stereochemistry	ACHIRAL
Molecular Formula	C15H9FN2
Molecular Weight	236.2438
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=NC(=CC=C1)C#CC2=CC(=CC(F)=C2)C#N

InChI

InChIKey=ZGEXQIMQZVRTDZ-UHFFFAOYSA-N

InChI=1S/C15H9FN2/c1-11-3-2-4-15(18-11)6-5-12-7-13(10-17)9-14(16)8-12/h2-4,7-9H,1H3

HIDE SMILES / InChI

Molecular Formula	C15H9FN2
Molecular Weight	236.2438
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21546249

MFZ 10-7 is a high affinity negative allosteric modulator at the mGlu5 receptor (Ki = 0.67 nM). MFZ 10-7 demonstrates anxyolitic properties in mouse models. Intraperitoneal administration of MFZ 10-7 inhibited intravenous cocaine self-administration, cocaine-induced reinstatement of drug-seeking behavior and cocaine-associated cue-induced cocaine-seeking behavior in rats.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Metabotropic glutamate receptor 5 39 Target ID: P41594 Gene ID: 2915.0 Gene Symbol: GRM5 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/21546249	Antagonist 2778		1.22 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Anxiety 267 Sources: https://www.ncbi.nlm.nih.gov/pubmed/21546249	Primary		Preclinical	Unknown Approved Use Unknown
Cocaine addiction 28 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24001208	Primary		Preclinical	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.	2011 Jun 1	21546249
Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation.	2012 Jul 12	22924094
A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats.	2014 Mar	24001208

Patents

Sample Use Guides

In Vivo Use Guide

For anxyolitic tests MFZ 10-7 was delivered via ip injection 15 min prior to testing. Anxyolitic effects were observed at dose 0.3 mg/kg.

Route of Administration: Intraperitoneal

In Vitro Use Guide

MFZ 10-7 was evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro assay. MFZ 10-7 (compound 2d) inhibited mGluR5 with IC50 1.22 nM.

Substance Class	Chemical Created by `admin` on `Sat Dec 16 17:36:09 UTC 2023` Edited by `admin` on `Sat Dec 16 17:36:09 UTC 2023`
Record UNII	FV36HKQ9RA
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

MFZ10-7

Code

English

3-Fluoro-5-[2-(6-methyl-2-pyridinyl)ethynyl]benzonitrile

Systematic Name

English

MFZ-10-7

Code

English

Benzonitrile, 3-fluoro-5-[2-(6-methyl-2-pyridinyl)ethynyl]-

Systematic Name

English

Code System Code Type Description

CAS

1224431-15-5