Home Neuronal Signaling 5-HT Receptor antagonist SB 271046 hydrochloride For research use only.

SB 271046 hydrochloride

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.

SB 271046 hydrochloride Chemical Structure

SB 271046 hydrochloride Chemical Structure

CAS No. 209481-24-3

Purity & Quality Control

Batch: S285601 DMSO]40 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.06%
99.06

SB 271046 hydrochloride Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

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
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
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]
Animal Research Animal Models Male Sprague Dawley rats
Dosages 30 mg/kg
Administration Orally

Chemical Information & Solubility

Molecular Weight 488.45 Formula

C20H22ClN3O3S2·HCl
CAS No. 209481-24-3 SDF Download SB 271046 hydrochloride SDF
Smiles CC1=C(SC2=C1C=C(C=C2)Cl)S(=O)(=O)NC3=CC(=C(C=C3)OC)N4CCNCC4.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 40 mg/mL ( (81.89 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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