Carabersat (Synonyms: SB-204269)

Cat. No.: HY-U00307: FAQs
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Carabersat is a potent anticonvulsant agent.

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Carabersat Chemical Structure

CAS No. : 184653-84-7

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Description	Carabersat is a potent anticonvulsant agent.
In Vitro	[³H]Carabersat ([³H]SB 204269) binds to rat forebrain membranes with moderate affinity (K_d 40 nM) and pK_i values of 7.3^[1]. Carabersat is able to bind to mouse forebrain membranes, and the binding is saturable and stereospecific, with a K_d of 53 nM. The labelled [³H]Carabersat produces a K_d 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Carabersat Related Antibodies
In Vivo	Carabersat (5b) significantly elevates anticonvulsant activity in mice^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight	357.38
Formula	C₂₀H₂₀FNO₄
CAS No.	184653-84-7
SMILES	O=C(N[C@@H]1[C@@H](O)C(C)(C)OC2=CC=C(C(C)=O)C=C12)C3=CC=C(F)C=C3
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (275 KB) Handling Instructions (2659 KB)
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. [Content Brief] [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. [Content Brief] [4]. Crespi F, et al. SB-204269 SmithKline Beecham. IDrugs. 1998 Sep;1(5):595-8. [Content Brief]

Animal Administration
^[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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. [Content Brief]

[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. [Content Brief]

[4]. Crespi F, et al. SB-204269 SmithKline Beecham. IDrugs. 1998 Sep;1(5):595-8. [Content Brief]

Carabersat Related Classifications

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Carabersat184653-84-7SB-204269SB204269SB 204269OthersInhibitorinhibitorinhibit

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Carabersat (Synonyms: SB-204269)

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