SB 271046 (Hydrochloride)
Modify Date: 2024-01-02 01:20:49
SB 271046 (Hydrochloride) structure
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Common Name | SB 271046 (Hydrochloride) | ||
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| CAS Number | 209481-24-3 | Molecular Weight | 488.45 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C20H23Cl2N3O3S2 | Melting Point | N/A | |
| MSDS | USA | Flash Point | N/A | |
Use of SB 271046 (Hydrochloride)SB271046 Hcl is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9.IC50 Value: 8.9(pKi)Target: 5-HT6 Receptorin vitro: SB 271046 hydrochloride is a sulfonamidal benzothiophene derivative that has been shown to act as a selective 5-HT6 antagonist with pKi values of 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 for 5-HT6, 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively, and is > 200-fold selective over 55 other receptors, enzymes and ion channels.in vivo: SB-271046 is moderately brain penetrant (10%), subject to low blood clearance (7.7 mL/min/kg) with a good half-life in rats (4.8 hours), and has excellent oral bioavailability (>80%). SB-271046 produces 3-fold and 2-fold increases in extracellular glutamate levels in both frontal cortex and dorsal hippocampus of rats, respectively, which may be used for the treatment of cognitive and memory dysfunction. SB-271046 (20 mg/kg, orally gavage) 30 min prior to training Wistar rats, is found to reverse significantly the amnesia produced by administering scopolamine (0.8 mg/kg, i.p.) in the 6 hours post-training period. SB-271046 progressively and significantly decreases platform swim angle and escape latencies over the five sequential trials on four consecutive daily sessions compared to vehicle-treated controls in aged rats. SB-271046 also improves task recall as measured by significant increases in the searching of the target quadrant on post-training days 1 and 3. SB-271046 (10 mg/kg, s.c.) produces a significant, tetrodotoxin-dependent, increase in extracellular levels of both glutamate and aspartate within the frontal cortex of rats, reaching maximum values of 375.4% and 215.3% of preinjection values, respectively. |
| Name | UNII:5346058Q7S |
|---|---|
| Synonym | More Synonyms |
| Description | SB271046 Hcl is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9.IC50 Value: 8.9(pKi)Target: 5-HT6 Receptorin vitro: SB 271046 hydrochloride is a sulfonamidal benzothiophene derivative that has been shown to act as a selective 5-HT6 antagonist with pKi values of 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 for 5-HT6, 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively, and is > 200-fold selective over 55 other receptors, enzymes and ion channels.in vivo: SB-271046 is moderately brain penetrant (10%), subject to low blood clearance (7.7 mL/min/kg) with a good half-life in rats (4.8 hours), and has excellent oral bioavailability (>80%). SB-271046 produces 3-fold and 2-fold increases in extracellular glutamate levels in both frontal cortex and dorsal hippocampus of rats, respectively, which may be used for the treatment of cognitive and memory dysfunction. SB-271046 (20 mg/kg, orally gavage) 30 min prior to training Wistar rats, is found to reverse significantly the amnesia produced by administering scopolamine (0.8 mg/kg, i.p.) in the 6 hours post-training period. SB-271046 progressively and significantly decreases platform swim angle and escape latencies over the five sequential trials on four consecutive daily sessions compared to vehicle-treated controls in aged rats. SB-271046 also improves task recall as measured by significant increases in the searching of the target quadrant on post-training days 1 and 3. SB-271046 (10 mg/kg, s.c.) produces a significant, tetrodotoxin-dependent, increase in extracellular levels of both glutamate and aspartate within the frontal cortex of rats, reaching maximum values of 375.4% and 215.3% of preinjection values, respectively. |
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| Related Catalog | |
| References |
| Molecular Formula | C20H23Cl2N3O3S2 |
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| Molecular Weight | 488.45 |
| Storage condition | -20℃ |
| RIDADR | NONH for all modes of transport |
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| 2,6-Piperazinedione, 4-[(1S)-2-(3,5-dioxo-1-piperazinyl)-1-methylethyl]-, hydrochloride (1:1) |
| 4,4'-(2S)-Propan-1,2-diyldipiperazin-2,6-dionhydrochlorid |
| 4,4'-(2S)-propane-1,2-diyldipipérazine-2,6-dione chlorhydrate |
| (S)-4,4'-(1-Methyl-1,2-ethanediyl)bis-2,6-piperazinedionehydrochloride |
| Dexrazoxane hydrochloride |
| 2,6-Piperazinedione, 4,4'-[(1S)-1-methyl-1,2-ethanediyl]bis-, hydrochloride (1:1) |
| 4,4'-[(2S)-1,2-Propanediyl]di(2,6-piperazinedione) hydrochloride (1:1) |
| 2,6-piperazinedione, 4,4'-[(1S)-1-methyl-1,2-ethanediyl]bis-, monohydrochloride |
| 4,4'-(2S)-Propane-1,2-diyldipiperazine-2,6-dione hydrochloride (1:1) |
| Dexrazoxane HCl |
| UNII:5346058Q7S |
| SB 271046 (Hydrochloride) |