1146414-35-8

Basic information

• Product Name: tetrahydropyran-4-carboxylic acid [((2S,3′S)-2-methyl[1,3′]bipyrrolidinyl-1′-yl)phenyl]amide
• Synonyms: tetrahydropyran-4-carboxylic acid [((2S,3′S)-2-methyl[1,3′]bipyrrolidinyl-1′-yl)phenyl]amide
• CAS NO: 1146414-35-8
• Molecular Weight: 371.523
• Mol File: 1146414-35-8.mol
• Article Data: 2

Chemical Properties

• CAS DataBase Reference: tetrahydropyran-4-carboxylic acid [((2S,3′S)-2-methyl[1,3′]bipyrrolidinyl-1′-yl)phenyl]amide(CAS DataBase Reference)
• NIST Chemistry Reference: tetrahydropyran-4-carboxylic acid [((2S,3′S)-2-methyl[1,3′]bipyrrolidinyl-1′-yl)phenyl]amide(1146414-35-8)
• EPA Substance Registry System: tetrahydropyran-4-carboxylic acid [((2S,3′S)-2-methyl[1,3′]bipyrrolidinyl-1′-yl)phenyl]amide(1146414-35-8)

Safety Data

• Hazardous Substances Data: 1146414-35-8(Hazardous Substances Data)

Upstream product

• 5337-03-1 tetrahydro-2H-pyran-4-carboxylic acid 
• 1056623-62-1 2-methyl-4-(2-(2S)-methyl-[1,3'(3'S)]bipyrrolidinyl-1'-yl)-phenylamine 

Relevant articles and documents

Discovery of a potent, selective, and orally bioavailable histamine H 3 receptor antagonist SAR110068 for the treatment of sleep-wake disorders

Previous studies have shown that compound 1 displayed high affinity towards histamine H3 receptor (H3R), (human (h-H3R), Ki = 8.6 nM, rhesus monkey (rh-H3R), Ki = 1.2 nM, and rat (r-H3R), Ki = 16.5 nM), but exhibited high affinity for hERG channel. Herein, we report the discovery of a novel, potent, and highly selective H3R antagonist/inverse agonist 5a(SS) (SAR110068) with acceptable hERG channel selectivity and desirable pharmacological and pharmacokinetic properties through lead optimization sequence. The significant awakening effects of 5a(SS) on sleep-wake cycles studied by using EEG recording in rats during their light phase support its potential therapeutic utility in human sleep-wake disorders.