SB-215505

Names

[ Name ]:
SB-215505

[Synonym ]:
HMS3262F03
Lopac-S-1068
6-Chloro-5-methyl-1-5-quinolycarbamoyl-indoline

Biological Activity

[Description]:

SB-215505 is a potent and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively[1]. SB-215505 increases wakefulness and motor activity in rats[2].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT2B Receptor:8.3 (pKi)

5-HT2A Receptor:6.77 (pKi)

5-HT2C Receptor:7.66 (pKi)

[In Vitro]

SB-215505 is 30 fold selective for the 5-HT2B over the 5-HT2A receptor, and only marginally selective over the 5-HT2C receptor[1].

[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]. 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.

[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.

[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.

Chemical & Physical Properties

[ Density]:
1.385g/cm3

[ Boiling Point ]:
600.9ºC at 760 mmHg

[ Molecular Formula ]:
C₁₉H₁₆ClN₃O

[ Molecular Weight ]:
337.80300

[ Flash Point ]:
317.2ºC

[ Exact Mass ]:
337.09800

[ PSA ]:
48.46000

[ LogP ]:
4.27810

[ Vapour Pressure ]:
2.13E-14mmHg at 25°C

[ Index of Refraction ]:
1.725

MSDS

Click to get detail MSDS

Safety Information

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

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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