| Name | SB-224289 hydrochloride |
| Description | SB-224289 hydrochloride (SB-224289A) is a selective antagonist of 5-HT1B receptor, with anxiolytic effect. |
| In vitro | SB-224289 demonstrates specific toxin-blocking properties without directly inhibiting the PS synthase enzyme or Cho1p in vitro. It consistently shows efficacy in producing Pap-A resistance at concentrations ranging from 100 μM to 25 μM and uniquely blocks the activity of papuamides, without affecting other membrane disruptors. Although SB-224289 does not protect wild-type cells from KF, it offers protection against TPap-A. It possesses a high affinity, with a pKi of 8, for human cloned 5-HT1B receptors, showing greater than 80-fold selectivity compared to the 5-HT1D receptor and other receptor types. As a potent antagonist (with a pEC50 of 7.9±0.1), SB-224289 induces a rightward shift in the 5-HT concentration response curve (with a pA2 of 8.4±0.2) and significantly enhances [3H]-5HT release in electrically stimulated guinea-pig brain cortex slices at 100 nM and 1 μM concentrations. |
| 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 8.33 mg/mL (14.95 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween-80+45% Saline : 0.5 mg/mL (0.9 mM), Sonication is recommended.
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| Keywords | SB-224289 Hydrochloride | SB224289 Hydrochloride | SB 224289 Hydrochloride | 5HTReceptor | 5-HT1B Receptor | 5-HT1B | 5HT Receptor |
| Inhibitors Related | Alverine citrate | Sevoflurane | Dapoxetine hydrochloride | Cefaclor monohydrate | Clozapine N-Oxide | 1,8-Cineole | Dopamine hydrochloride | Cloperastine hydrochloride | Mianserin hydrochloride | Trazodone hydrochloride | Cinchonidine | Doxepin hydrochloride |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Anti-Alzheimer's Disease Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Angiogenesis related Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Serotonin Receptor-Targeted Compound Library |
United States
