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.
Drug Discovery Research Laboratory, Sanwa Kagaku Kenkyusho Co., Ltd., Mie, Japan.
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T
Suzuki
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Inagaki
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H
Hamajima
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H
Uesaka
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Hori
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T
Ikami
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