Comparison of basicity and lipophilicity of 8 nicotinic receptor blockers: Quinuclidines and Piperidines



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Comparison of basicity and lipophilicity of 8 nicotinic receptor blockers: Quinuclidines and Piperidines.
 


 
Products
Code		 pKa[1]
(H2O, 30°C)		 % of cationic
form (pH 7.4)		 log p (octanol-water)[2]
neutral form		 p' (octanol-water)[3]
pH 7.4		 Lipophilic
membrane
penetration[4]		 Stable TEMPO
radical
NANOPHINE L9042 10.99 99.97% 1.82 0.02 high +/-
PEMPIDINE L9043 11.25 98.98% 3.29 0.27 high No
PEMPIDONE L9067 7.95[5] 78.01% 2.28 41.90 high No
QUIRESTINE L9045 - 100% at any pH - ~0 low No
TEMECHINE L9044 >11.20[5] >99.98% 3.44 ~0.55 high No
TEMPIDINE[4] L9059 11.05 99.98% 2.86 0.16 high Yes
TEMPIDONE[4] L9046 7.80[5] 71.52% 1.85 20.16 high Yes
TEMPOXIME[4] L9057 8.95[5] 97.26% 0.09 0.03 high Yes


[1] Hall, J.Am.Chem.Soc. 79(20):5444-5447 (1957).

[2] Calculated according to Rekker and Manhold, "Calculation of drugs lipophilicity: the hydrophobic fragmental constant approach", Weinheim (1992).

[3] p'=[%neutral form x pn.(calc.)+ % cationic form x pcat.(calc.)]/100

[4] TEMP derivatives are also antioxidants due to the conversion of "hot" oxygen-containing radicals into stable TEMPO radicals.


[5] Data to be published.

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