Chemical Property of Intepirdine
Chemical Property:
- Boiling Point:608.3±45.0 °C(Predicted)
- PKA:8?+-.0.10(Predicted)
- PSA：70.68000
- Density:1.292
- LogP:3.95180
- Solubility.:insoluble in H2O; ≥17.65 mg/mL in DMSO; ≥2.13 mg/mL in EtOH with gentle warming and ultrasonic
- XLogP3:2.5
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:5
- Rotatable Bond Count:3
- Exact Mass:353.11979803
- Heavy Atom Count:25
- Complexity:535
- Purity/Quality:
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99%, *data from raw suppliers
3-(Phenylsulfonyl)-8-(piperazin-1-yl)quinoline 95% *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:C1CN(CCN1)C2=CC=CC3=CC(=CN=C32)S(=O)(=O)C4=CC=CC=C4
- Recent ClinicalTrials:Study Evaluating Intepirdine (RVT-101) on Gait and Balance in Subjects With Dementia
- Recent EU Clinical Trials:A Long-Term Extension Study of the Safety and Tolerability of RVT-101 in Subjects with Dementia with Lewy Bodies (DLB)
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Description
SB-742457 is an orally bioavailable antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 1.4 nM). SB-742457 (1 μM) also binds to 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors with high affinity. SB-742457 reduces 5-HT6 activation of Gs-mediated cAMP production in a concentration-dependent manner with an EC50 value of 21 nM in NG108-15 neuroblastoma cells. In vivo, SB-742457 (1.5 mg/kg, p.o.) reverses deficits in novel object recognition induced by scopolamine in rats. It also reverses age-induced impairments in spatial memory acquisition and retention in rats in the Morris water maze. SB-742457 (3.0 mg/kg, i.p.) reduces the number of licking bouts by 24% compared with control in rats trained to lick a glucose solution, indicating a role in satiety and obesity management.
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Uses
SB 742457 is a selective 5-HT6 receptor antagonist which is known to be involved in improving cognitive function.
