2-(4-R-phenoxy/phenylthio)alkanoic esters of l-lupinine.
Considering the great pharmacological interest in phenoxy/phenylthioalkanoic esters of open-chain or cyclic aminoalcohols, a set of ten such esters of lupinine was prepared. Initially, their ability to displace [3H]QNB from rat brain preparation was investigated. With the exception of two, all the prepared esters exhibited good affinity to muscarinic receptors (on a non-selective basis), with pKi in the range 6.67-7.68.
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Istituto di Chimica Farmaceutica e Tossicologica, University of Milan, Viale Abruzzi, 42-I-20131 Milan, Italy. anna.sparatore@unimi.it
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D000470:Alkaloids / Q000737:chemistry*; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004952:Esters; D066298:In Vitro Techniques; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D018727:Muscarinic Antagonists / Q000493:pharmacokinetics; D011813:Quinuclidinyl Benzilate / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D011976:Receptors, Muscarinic / Q000187:drug effects / Q000378:metabolism; D013034:Sparteine / Q000031:analogs & derivatives; D013055:Spectrophotometry, Infrared; D000093843:Quinolizidine Alkaloids
D000470:Alkaloids; D004952:Esters; D008024:Ligands; D018727:Muscarinic Antagonists; D011813:Quinuclidinyl Benzilate; D011976:Receptors, Muscarinic; D013034:Sparteine; C015971:lupinine; D000093843:Quinolizidine Alkaloids