SB 224289 HYDROCHLORIDE
SB 224289 HYDROCHLORIDE Basic information
- Product Name:
- SB 224289 HYDROCHLORIDE
- Synonyms:
-
- 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4'-piperidine] hydrochloride
- SB-224289A, 1μ-Methyl-5-[[2μ-methyl-4μ-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4μ-piperidine] hydrochloride
- SB 224289A
- (2'-Methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)(1'-methyl-6,7-dihydrospiro[furo[2,3-f]indole-3,4'-piperidin]-5(2H)-yl)methanone hydrochloride
- SB-224289 hydrochloride, 10 mM in DMSO
- CAS:
- 180084-26-8
- MF:
- C32H32N4O3HCl
- MW:
- 0
- Mol File:
- 180084-26-8.mol
SB 224289 HYDROCHLORIDE Chemical Properties
- storage temp.
- Store at RT
- solubility
- Soluble to 10 mM in DMSO with gentle warming
- form
- Powder
- color
- White to off-white
Safety Information
- Safety Statements
- 22-24/25
SB 224289 HYDROCHLORIDE Usage And Synthesis
Uses
SB 224289A is a 5-HT1B antagonist.
Uses
SB-224289 Hydrochloride is a selective SR-1B antagonist; 5-HT1B antagonist.
Definition
ChEBI: SB 224289 hydrochloride is a hydrochloride that is the monohydrochloride salt of SB 224289. Selective 5-HT1B receptor antagonist (pKi = 8.2). Displays >60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C receptors in radioligand binding and functional assays. Centrally active following oral administration in vivo. It has a role as a prodrug and a serotonergic antagonist. It contains a SB 224289(1+).
in vivo
SB-224289 (SB 224289) alone or in combination with cocaine, increases anxiety-like behavior. SB 224289 significantly reduces the amount of locomotor activity in the cocaine-treated rats. SB 224289-treated animals spend a significantly longer time in the corners than those treated with vehicle[2]. SB 224289 is a potent antagonist with an ED50 of 3.6 mg/kg, p.o in SK&F-99101-induced hypothermia in the guinea-pig. SB 224289 (4 mg/kg, p.o) reverses sumatriptan-induced inhibition of 5-HT release showing that it is also a potent terminal 5-HT autoreceptor antagonist in vivo. SB 224289 (2-16 mg/kg, p.o) does not increase 5-HT levels in the fuinea-pig frontal cortex. However, SB 224289 (4 mg/kg, p.o) causes a significantly increase in levels of 5-HT in the fuinea-pig dentate gyrus[3].
IC 50
5-HT1B Receptor
storage
Room temperature
SB 224289 HYDROCHLORIDESupplier
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