The intrinsic alpha activities and the D2 (frog, m, rectus abdominalis) concentrations were estimated for different acetylcholine and sebacinylcholine derivatives. So were also the A2 values for ...antagonists and the affinity constants Kc for some partial agonists. The results obtained disprove Paton's "rate-theory". The relationship between the cholinergic activity and the volume of cationic groups was studied and it could not possibly be explained by the steric hindrance alone. It is suggested that certain hydrophobic radicals of the cationic groups contact the receptor surface outside the anionic centre. Such contacts prevent the cholinoreceptor to change its conformation and thus inhibit the depolarization of the membrane. An approximate estimation of the anionic site dimensions is given.
Tercuronium is p',p"-bis-triethylammonium-p-terphenyl dibenzosulfonate. As a curarelike agent tercuronium is 4--8 times as potent as (+)-tubocurarine. The time of the development and lasting of the ...blocking effect of tercuronium is approximately the same as that of (+)-tubocurarine. In a blocking dose tercuronium does not exert any effect either on the vegetative ganglia or arterial blood pressure. Partial blocking of the transmission through the vegetative ganglia as well as an insignificant and short-term drop of arterial blood pressure are recorded after intravenous injection of 10 myoparalytic doses of tercuronium. The antagonism of neostigmine against tercuronium was more pronounced than against (+)-tubocurarine, pancuronium and gallamine.
Detection of malaria in the USSR, 1967-1970 Dukhanina, N N; Sarikian, S Ia; Zhukova, T A ...
Meditsinskaia parazitologiia i parazitarnye bolezni,
1972 May-Jun, Letnik:
41, Številka:
3
Journal Article