Synthesis and biological activity of the metabolites of N-[2-(1-azabicyclo[3.3.0]octan-5-yl)ethyl]-2-nitroaniline fumarate (SK-946).
Three metabolites of N-[2-(1-azabicyclo[3.3.0]octan-5-yl)ethyl]-2-nitroaniline fumarate (SK-946), a novel central muscarinic cholinergic receptor agonist, were prepared to confirm their proposed structures, and tested for muscarinic receptor affinity in vitro.
Suzuki
T
T
Drug Discovery Research Laboratory, Sanwa Kagaku Kenkyusho Co., Ltd., Mie, Japan.
Inagaki
H
H
Hamajima
H
H
Uesaka
H
H
Hori
K
K
Ikami
T
T
D000814:Aniline Compounds / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects; D001643:Bridged Bicyclo Compounds / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D002855:Chromatography, Thin Layer; D066298:In Vitro Techniques; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D018721:Muscarinic Agonists / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D018727:Muscarinic Antagonists / Q000493:pharmacokinetics; D010890:Pirenzepine / Q000493:pharmacokinetics; D011813:Quinuclidinyl Benzilate / Q000493:pharmacokinetics; D051381:Rats; D043643:Receptor, Muscarinic M1; D043585:Receptor, Muscarinic M2; D011976:Receptors, Muscarinic / Q000187:drug effects / Q000378:metabolism
D000814:Aniline Compounds; D001643:Bridged Bicyclo Compounds; D018721:Muscarinic Agonists; D018727:Muscarinic Antagonists; C107666:N-(2-(1-azabicyclo(3.3.0)octan-5-yl)ethyl)-2-nitroaniline; D043643:Receptor, Muscarinic M1; D043585:Receptor, Muscarinic M2; D011976:Receptors, Muscarinic; D010890:Pirenzepine; D011813:Quinuclidinyl Benzilate