2001
DOI: 10.1208/ps030430
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Receptor binding studies of soft anticholinergic agents

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Cited by 36 publications
(29 citation statements)
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“…A number of such compounds derived from methylatropine (e.g., PcPATR_NA.Me 104a, 104b) [302,303] or glycopyrrolate (e.g., PcPOAGP_NA.Et 104c) [304][305][306][307][308][309] have been recently synthesized and tested. Several of them showed promising and stereospecific in vitro receptor-binding and in vivo mydriatic activities as well as some degree of and M 3 /M 2 muscarinic-receptor subtype-selectivity.…”
Section: Soft Estrogensmentioning
confidence: 99%
“…A number of such compounds derived from methylatropine (e.g., PcPATR_NA.Me 104a, 104b) [302,303] or glycopyrrolate (e.g., PcPOAGP_NA.Et 104c) [304][305][306][307][308][309] have been recently synthesized and tested. Several of them showed promising and stereospecific in vitro receptor-binding and in vivo mydriatic activities as well as some degree of and M 3 /M 2 muscarinic-receptor subtype-selectivity.…”
Section: Soft Estrogensmentioning
confidence: 99%
“…46 Ovality is also an indicator of how close the molecule's geometry is to a sphere, a cylinder or a disk. 47 An Ov value of 1.0 means that the molecule is a perfect sphere. Cylindrical and disk-like molecules will have Ov values greater than and less than 1.0, respectively.…”
Section: Prediction By Mlrmentioning
confidence: 99%
“…The distribution coefficient of ionizable or permanently charged compounds was calculated by the QLogP software and by including a À3 Â 0.723 correction for primary amines compared to their neutral form and a À9 Â 0.723 contribution for quaternary ammonium compounds as described previously. [40][41][42] For the ionizable amines, experimental log D o/w values were also collected from the compilation by Hansch and co-workers 8 for verification of the predicted values. Anticholinergic activities are pA 2 values determined with the in vitro guinea pig ileum assay.…”
Section: Datamentioning
confidence: 99%
“…For example, the antimicrobial activity of straight-chain aliphatic amines (1-butanamine to 1-octadecanamine) against Rhinocladium beurmanni 32,38 and the antimicrobial activity of quaternary ammonium-containing L-carnitine double ester soft antimicrobials [RCOOCH(CH 2 COOR 0 )CH 2 -Nme 3 þ ] against Staphylococcus aureaus 39 are shown in Figures 6 and 7, respectively as a function of molecular volume V and the QLogP calculated log octanolwater distribution coefficient (log D o/w ), 41,42 which are linearly related (QLogP ¼ 0.032VÀ0.723N) and, hence, interchangeable on these congener series, where N, a hydrogen-bonding-related parameter, has a fixed value. Both data show bilinear behavior, but their maxima appear at considerably different V values.…”
Section: Antimicrobial Activitiesmentioning
confidence: 99%
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