Huang F, Buchwald P, Browne CE, Farag HH, Wu WM, Ji F, Hochhaus G and Bodor N Receptor Binding Studies of Soft Anticholinergic Agents AAPS PharmSci 2001;
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article 30
(https://www.pharmsci.org/scientificjournals/pharmsci/journal/01_30.html).
Figures and Tables
Figure 1.Synthesis of ethyl tropyl 3-thienylmalonate methosulfate salt (TMTR.Et, 4a ) and isopropyl tropyl 3-thienylmalonate methoiodide salt (TMTR.iPr, 4b ).
Figure 2.Synthesis of di-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl) phenylmalonate dimethiodide (PMTR.TR, 10a ) and di-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl) phenylsuccinate dimethiodide (PSTR.TR, 10b ).
Table 1.
Binding parameters of reference compounds at 4 muscarinic receptor subtypes. The affinity estimates were derived from [3H]NMS displacement experiments and represent the mean (ąSEM, n = 3-5) for the negative logarithm of Ki; Hill coefficients are given in parentheses.
Figure 3.Correlation between pA 2 and pK i (m3 ) data for soft anticholinergics.
Figure 4.Correlation between experimental and fitted (eq. 6, Table 8 ) pK i (m3 ) values.
Table 2.
Binding parameters of soft anticholinergics at m1, m2, m3, and m4 receptors. The affinity estimates were derived from [3H]NMS displacement experiments and represent the mean (ąSEM, n = 3-5) for the negative logarithm of Ki; Hill coefficients are given in parentheses.
Table 3.
Binding parameters of soft anticholinergics at m1, m2, m3, and m4 receptors. The affinity estimates were derived from [3H]NMS displacement experiments and represent the mean (ąSEM, n = 3-5) for the negative logarithm of Ki; Hill coefficients are given in parentheses.
Table 4.
Soft anticholinergicsa with a tropine moiety in their structure.
Table 5.
Soft anticholinergics with no tropine moiety in their structure.
Table 6.
Reference compounds used to obtain predicted log distribution coefficient (log D) with the QLogP method.
Table 7.
Selected physicochemical parameters for Soft anticholinergicsa containing a tropine moiety in their structure.
Table 8.
Regression equations.
Table 9.
Correlation matrix between selected physicochemical descriptors and pKi values.
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