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SB 228357

Names

[ CAS No. ]:
181629-93-6

[ Name ]:
SB 228357

[Synonym ]:
Tocris-1375
Lopac-S-2318

Biological Activity

[Description]:

SB228357 is a selective, potent oral active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects[1][2].

[Target]

5-HT2A Receptor:6.9 (pKi)

5-HT2C Receptor:9 (pKi)

5-HT2B Receptor:8 (pKi)


[In Vivo]

SB228357 (0-10 mg/kg; oral administration; for 90 minutes; male Sprague Dawley rats) treatment significantly reverses Haloperidol-induced catalepsy[2]. Animal Model: Male Sprague Dawley rats (200-250 g) injected with Haloperidol[2] Dosage: 0 mg/kg, 0.32 mg/kg, 1 mg/kg, 3.2 mg/kg, 10 mg/kg Administration: Oral administration; for 90 minutes Result: Significantly reversed Haloperidol-induced catalepsy.

[References]

[1]. Bromidge SM, et al. Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent. J Med Chem. 2000 Mar 23;43(6):1123-34.

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

Chemical & Physical Properties

[ Density]:
1.398g/cm3

[ Boiling Point ]:
625.4ºC at 760mmHg

[ Molecular Formula ]:
C22H17F4N3O2

[ Molecular Weight ]:
431.38300

[ Flash Point ]:
332ºC

[ Exact Mass ]:
431.12600

[ PSA ]:
54.46000

[ LogP ]:
5.64770

[ Vapour Pressure ]:
1.48E-15mmHg at 25°C

[ Index of Refraction ]:
1.599

Safety Information

[ Safety Phrases ]:
22-24/25

[ WGK Germany ]:
3

Related Compounds