2-(4-R-phenoxy/phenylthio)alkanoic esters of l-lupinine

A Sparatore; F Sparatore

doi:10.1016/s0014-827x(01)01036-9

2-(4-R-phenoxy/phenylthio)alkanoic esters of l-lupinine

Farmaco. 2001 Mar;56(3):169-74. doi: 10.1016/s0014-827x(01)01036-9.

Authors

A Sparatore¹, F Sparatore

Affiliation

¹ Istituto di Chimica Farmaceutica e Tossicologica, University of Milan, Viale Abruzzi, 42-I-20131 Milan, Italy. anna.sparatore@unimi.it

PMID: 11409323
DOI: 10.1016/s0014-827x(01)01036-9

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Alkaloids / chemistry*
Animals
Binding, Competitive / drug effects
Brain Chemistry / drug effects
Chemical Phenomena
Chemistry, Physical
Esters
In Vitro Techniques
Ligands
Magnetic Resonance Spectroscopy
Male
Muscarinic Antagonists / pharmacokinetics
Quinuclidinyl Benzilate / pharmacokinetics
Rats
Rats, Wistar
Receptors, Muscarinic / drug effects
Receptors, Muscarinic / metabolism
Sparteine / analogs & derivatives
Spectrophotometry, Infrared

Substances

Alkaloids
Esters
Ligands
Muscarinic Antagonists
Receptors, Muscarinic
Sparteine
lupinine
Quinuclidinyl Benzilate