Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SB-224289 hydrochloride (SB-224289A) is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 34.00 | |
5 mg | In stock | $ 80.00 | |
10 mg | In stock | $ 128.00 | |
25 mg | In stock | Inquiry | |
50 mg | In stock | Inquiry | |
1 mL * 10 mM (in DMSO) | In stock | $ 97.00 |
Description | SB-224289 hydrochloride (SB-224289A) is a selective antagonist of 5-HT1B receptor, with anxiolytic effect. |
In vitro | SB-224289 does not directly inhibit the PS synthase enzyme in this in vitro assay.SB-224289 has specific toxin-blocking ability and does not inhibit Cho1p. SB-224289 (100 μM-25 μM) shows consistent efficacy at producing Pap-A resistance. Moreover, SB-224289 specifically blocks the activity of papuamides and not other membrane disruptors. SB-224289 is unable to protect wild-type cells against KF, but it is able to provide protection against TPap-A[1]. SB-224289 has a pKi of 8 at human cloned 5-HT1B receptors and displays more than 80 fold selectivity over the closely related 5-HT1D receptor and a range of other receptors. SB-224289 is a potent antagonist(pEC50 of 7.9±0.1). SB-224289 evokes a parallel rightward shift in the 5-HT concentration response curve with pA2 of 8.4±0.2. SB-224289 (100 nM and 1 μM) also significantly increases [3H]-5HT release in electrically stimulated guinea-pig brain cortex slices[3]. |
In vivo | 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]. |
Synonyms | SB-224289A |
Molecular Weight | 557.08 |
Formula | C32H33ClN4O3 |
CAS No. | 180084-26-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 8.1mg/mL (14.5mM), ultrasonic and warming and heat to 60°C
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SB-224289 hydrochloride 180084-26-8 GPCR/G Protein Neuroscience 5-HT Receptor SB 224289 Hydrochloride SB-224289 Hydrochloride SB-224289A SB224289 Hydrochloride inhibitor inhibit