SB 271046 hydrochloride

Catalog No.S2856

SB 271046 hydrochloride Chemical Structure

Molecular Weight(MW): 488.45

SB 271046 hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 147 In stock
USD 570 In stock
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1 Customer Review

  • The levels of Aβ produced by SK-N-SH cells in response to the indicated HTR6 antagonists at 1μM, 3μM or 10μM for 24hours

    Sci Rep, 2017 , 7(1):4983. SB 271046 hydrochloride purchased from Selleck.

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Biological Activity

Description SB 271046 hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes.
Targets
5-HT6 [1]
(Cell-free assay)
8.92(pKi)
In vitro

SB-271046 also potently displaces [125I]-SB-258585 from rat and pig striatal and human caudate putamen membranes with pKis of 9.02, 8.55 and 8.81, respectively. SB-271046 competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71. [1] SB-271046 is found to be a competitive antagonist with a pA2 of 8.7 in the functional adenylyl cyclase assay which is in good agreement with its binding affinity. SB-271046 demonstrates no significant inhibitory activity at the major human P450 enzymes. [2]

In vivo SB-271046 produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of 0.1 mg/kg p.o. and maximum effect at 4 hours post-dose. The level of anticonvulsant activity achieves correlated well with the blood concentrations of SB-271046 (EC50 of 0.16 μM) and brain concentrations of 0.01 μM–0.04 μM at Cmax. [1] 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%). [2] 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. [3] 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. [4] 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. [5]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Male Sprague Dawley rats
  • Formulation: 1% methyl cellulose in water
  • Dosages: 30 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 40 mg/mL (81.89 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
1% methylcellulose
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 488.45
Formula

C20H22ClN3O3S2·HCl

CAS No. 209481-24-3
Storage powder
Synonyms N/A

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5-HT Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID