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Merck
CN

SML0249

βCCt

≥98% (HPLC)

别名:

β-Carboline-3-carboxylate-t-Bu ester, beta-Carboline-3-carboxylate-t-butyl ester, tert-Butyl β-carboline-3-carboxylate

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关于此项目

经验公式(希尔记法):
C16H16N2O2
化学文摘社编号:
分子量:
268.31
UNSPSC Code:
12352200
PubChem Substance ID:
MDL number:
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产品名称

βCCt, ≥98% (HPLC)

InChI

1S/C16H16N2O2/c1-16(2,3)20-15(19)13-8-11-10-6-4-5-7-12(10)18-14(11)9-17-13/h4-9,18H,1-3H3

SMILES string

CC(C)(C)OC(=O)c1cc2c(cn1)[nH]c3ccccc23

InChI key

FVFFDKKTXYVCCW-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: ≥10 mg/mL

storage temp.

2-8°C

Biochem/physiol Actions

βCCt has been characterized as an α1selective antagonist and benzodiazepine mixed agonist/antagonist.. A recent study found Ki values for the GABA-A subtypes were 0.72, 15, 18.9, 110.8, and >5,000 nM at five recombinant GABAA/BzR subtypes α1, α2, α3, α5, and α6 respectively. βCCt was a near ‘neutral′ antagonist (i.e., little or no efficacy) at all these 5 recombnant GABAA/BzR receptor subtypes. βCCt has been shown to reduce alcohol self-administration in alcohol preferring (P) and high alcohol drinking (HAD) rats.
βCCt is a GABBA antagonist selective for α1 subtype and a mixed benzodiazepine agonist-antagonist

Features and Benefits

This compound is featured on the GABAA Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

存储类别

13 - Non Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Donna M Platt et al.
Psychopharmacology, 164(2), 151-159 (2002-10-31)
Delineation of the receptor mechanisms underlying the behavioral effects of benzodiazepines should allow for the development of drugs with improved clinical utility and reduced side effects. OBJECTIVES. The purpose of the present study was to investigate the role of GABAA/alpha1
Christiaan H Vinkers et al.
Psychopharmacology, 204(2), 299-311 (2009-01-27)
The stress-induced hyperthermia (SIH) model is an anxiety model that uses the transient rise in body temperature in response to acute stress. Benzodiazepines produce anxiolytic as well as sedative side effects through nonselective binding to GABA(A) receptor subunits. The GABA(A)
Miroslav M Savić et al.
Psychopharmacology, 180(3), 455-465 (2005-02-19)
The pharmacological approach, using subtype selective ligands, complements genetic studies on the specific contribution of individual receptor subtypes to the various effects of benzodiazepines. The aim of this study was to examine the relative significance of alpha1-containing GABA(A) receptors in
Miroslav M Savić et al.
Pharmacology, biochemistry, and behavior, 79(2), 279-290 (2004-10-27)
Recent research using genetically modified mice has pointed to the specific contribution of individual receptor subtypes to the various effects of benzodiazepines. The aim of this study was to examine the relative significance of alpha(1)-containing GABA(A) receptors in the effects
Katrina L Foster et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 29(2), 269-284 (2003-12-11)
The present study tested the hypothesis that GABA(A) and opioid receptors within the central nucleus of the amygdala (CeA) regulate ethanol (EtOH), but not sucrose-maintained responding. To accomplish this, betaCCt, a mixed benzodiazepine (BDZ) agonist-antagonist with binding selectivity at the

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