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FG 7142

Names

[ CAS No. ]:
78538-74-6

[ Name ]:
FG 7142

[Synonym ]:
B-carboline-3-carboxylic acid N-*methylamide
FG 7142

Biological Activity

[Description]:

FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[In Vitro]

FG-7142 has affinity for those expressing the α subunit, the Ki values are 91 nM; 330 nM; 492 nM and 2.150 μM for α1, α2,α3 and α5 subunits, respectively[1]. FG-7142 has a high efficacy in modulating GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50 = 137 nM) as compared to the other α subunits (EC50: α2= 507 nM,α3=1.021μM , α5=1.439 μM)[1].

[In Vivo]

FG-7142 (intraperitoneal injection; 15-30 mg/kg) activates mesolimbocortical dopaminergic projections, leading to increases in dopamine in the prefrontal cortex and the nucleus accumbens in rats[1]. FG-7142 (intraperitoneal injection; 15 mg/kg) increases tyrosine hydroxylase activity and dopamine turnover in the medial prefrontal cortex and ventral tegmentum in vivo, but effects are not detected in mesolimbic or nigrostriatal areas[1].

[References]

[1]. Cottone P, et al. FG 7142 specifically reduces meal size and the rate and regularity of sustained feeding in female rats: evidence that benzodiazepine inverse agonists reduce food palatability.Neuropsychopharmacology. 2007 May;32(5):1069-81. Epub 2006 Nov 1.

Chemical & Physical Properties

[ Density]:
1.328g/cm3

[ Boiling Point ]:
576.3ºC at 760 mmHg

[ Molecular Formula ]:
C13H11N3O

[ Molecular Weight ]:
225.24600

[ Flash Point ]:
302.3ºC

[ Exact Mass ]:
225.09000

[ PSA ]:
57.78000

[ LogP ]:
2.46660

[ Index of Refraction ]:
1.735

[ Storage condition ]:
2-8°C

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UU9780100
CHEMICAL NAME :
9H-Pyrido(3,4-b)indole-3-carboxamide, N-methyl-
CAS REGISTRY NUMBER :
78538-74-6
LAST UPDATED :
199212
DATA ITEMS CITED :
1
MOLECULAR FORMULA :
C13-H11-N3-O
MOLECULAR WEIGHT :
225.27

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
150 mg/kg
SEX/DURATION :
female 12-21 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
GEPHDP General Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.6- 1975- Volume(issue)/page/year: 22,53,1991

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ RTECS ]:
UU9780100

[ HS Code ]:
2933990090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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