SB-215505

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SB-215505 is a potent and subtype-selective 5-HT_2B receptor antagonist with pK_i values of 8.3, 6.77, 7.66 for 5-HT_2B, 5-HT_2A, 5-HT_2C, respectively. SB-215505 increases wakefulness and motor activity in rats.

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SB-215505 Chemical Structure

CAS No. : 162100-15-4

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Description

SB-215505 is a potent and subtype-selective 5-HT_2B receptor antagonist with pK_i values of 8.3, 6.77, 7.66 for 5-HT_2B, 5-HT_2A, 5-HT_2C, respectively^[1]. SB-215505 increases wakefulness and motor activity in rats^[2].

IC₅₀ & Target^[1]

5-HT_2B Receptor

8.3 (pKi)

5-HT_2A Receptor

6.77 (pKi)

5-HT_2C Receptor

7.66 (pKi)

In Vitro

SB-215505 is 30 fold selective for the 5-HT_2B over the 5-HT_2A receptor, and only marginally selective over the 5-HT_2C receptor^[1].

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

In Vivo

SB-215505 (0.1-1.0 mg/kg; i.p.; two doses) dose-dependently increases wakefulness (W) and decreases IS, PS, SWS-2^[2].

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

Animal Model:	Male Sprague-Dawley rats weighing 230-260 g^[2]
Dosage:	0.1, 0.3 and 1.0 mg/kg
Administration:	IP; two doses (4 days between two doses)
Result:	Dose-dependently increased wakefulness (W) and decreased intermediate stage of sleep (IS), paradoxical sleep (PS), SWS-2.

Molecular Weight

337.80

Formula

C₁₉H₁₆ClN₃O

CAS No.

162100-15-4

SMILES

O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=C4C=CC=NC4=CC=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

Handling Instructions (2659 KB)

References

[1]. C Reavill, et al. Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol. 1999 Feb;126(3):572-4. [Content Brief]

[2]. Sandor Kantor, et al. Increased wakefulness, motor activity and decreased theta activity after blockade of the 5-HT2B receptor by the subtype-selective antagonist SB-215505. J Pharmacol. 2004 Aug;142(8):1332-42. [Content Brief]

SB-215505 Related Classifications

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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.

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