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[Effect of pH on muscarinic antagonist selectivity]
A B Kosmachev1, M B Iakhontova, T A Titkova
1Institute of Toxicology, Ministry of Public Health of the Russian Federation, ul. Bekhtereva 1, St. Petersburg, 193019 Russia.
Abstract:
The results of in vitro experiments showed that the receptor selectivity of the M-cholinoblocker tropacin (in contrast to that of amedine) is pH-dependent. A difference observed in the characteristics of tropacin selectivity in vivo and in vitro is probably explained by dissimilar conditions for the ligand interaction with M-cholinoreceptors in the organism and in the in vitro experiments. It is suggested that certain short-time (transient) local pH changes capable of affecting the ligand--receptor interaction parameters may take place in the synaptic cleft in the course of the neurotransmission.