Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Carabersat?
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Purity: 98.0%
Stocking Period: 10 Day
Contact: Yang

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Carabersat
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

184653-84-7

184653-84-7 structure

184653-84-7 structure

Name: Carabersat
Chemical Name: (3R,4S)-6-Acetyl-4-(4-fluorobenzamido)-3,4-dihydro-2,2-dimethyl-3-hydroxy-2H-1-benzopyran
CAS Number: 184653-84-7
Molecular Formula: C₂₀H₂₀FNO₄
Molecular Weight: 357.37600
Catalog: Research Areas Neurological Disease
Create Date: 2016-11-13 14:10:20
Modify Date: 2024-01-09 17:56:08
Carabersat is a potent anticonvulsant agent.

Name	(3R,4S)-6-Acetyl-4-(4-fluorobenzamido)-3,4-dihydro-2,2-dimethyl-3-hydroxy-2H-1-benzopyran
Synonyms	carabersat CARABERSAT trans-4-(4-fluorobenzoylamino)-6-acetyl-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3-ol trans-(+)-6-acetyl-4S-(4-fluorobenzoylamino)-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-3R-ol trans-(+)-6-acetyl-4S-(4-fluorobenzoylamino)-3,4-dihydro-2,2-dimethyl-2H-benzo[b]pyran-3R-ol

Description	Carabersat is a potent anticonvulsant agent.
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Neurological Disease
In Vitro	[3H]Carabersat ([3H]SB 204269) binds to rat forebrain membranes with moderate affinity (Kd 40 nM) and pKi values of 7.3[1]. Carabersat is able to bind to mouse forebrain membranes, and the binding is saturable and stereospecific, with a Kd of 53 nM. The labelled [3H]Carabersat produces a Kd of 32 nM[2]. Carabersat (SB-204269, 1-100 μM) has no effect on Na+ current in cultured hippocampal neurones. Carabersat also shows no effect on action potential discharges evoked by elevating external K+[3]. Carabersat (SB-204269) is structurally-related to the benzopyran ATP-sensitive potassium channel (KATP) opener, cromakalim, but has opposite stereochemistry, and the mechanism of action of Carabersat is not thought to involve KATP[4].
In Vivo	Carabersat (5b) significantly elevates anticonvulsant activity in mice[1].
Animal Admin	Mice[1] In this model, groups of 10-20 naive mice (25-30 g) are assessed for production of a tonic hindlimb extension seizure following a single corneal electroshock using an "up and down" method of shock titration. The effects of drug treatment are expressed as a percentage change from vehicle control values and statistical comparisons between groups are made. Carabersat is administered orally as a fine suspension in 1% methylcellulose one hour before electroshock application[1].
References	[1]. Wai N. Chan, et al. Synthesis of Novel trans-4-(Substituted-benzamido)-3,4-dihydro-2H-benzo[b]pyran-3-ol Derivatives as Potential Anticonvulsant Agents with a Distinctive Binding Profile. J. Med. Chem., 1996, 39 (23), pp 4537-4539. [2]. Herdon H, et al. The novel anticonvulsant SB 204269 binds to a stereospecific site in the mouse brain. Eur J Pharmacol. 1996 Oct 31;314(3):R7-8. [3]. Caeser M, et al. Lack of effect of the novel anticonvulsant SB-204269 on voltage-dependent currents in neurones cultured from rat hippocampus. Neurosci Lett. 1999 Aug 13;271(1):57-60. [4]. Crespi F, et al. SB-204269 SmithKline Beecham. IDrugs. 1998 Sep;1(5):595-8.

Molecular Formula	C₂₀H₂₀FNO₄
Molecular Weight	357.37600
Exact Mass	357.13800
PSA	75.63000
LogP	3.42220
Storage condition	2-8℃