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The stereospecificity of LY253352 for α 1 ‐adrenoceptor binding sites in the brain and prostate
Author(s) -
Lepor Herbert,
Baumann Mary,
Shapiro Ellen
Publication year - 1988
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1988.tb16557.x
Subject(s) - dissociation constant , radioligand , enantiomer , human brain , chemistry , stereospecificity , prostate , adenoma , endocrinology , antagonist , alpha (finance) , receptor , medicine , stereochemistry , biology , neuroscience , biochemistry , patient satisfaction , construct validity , cancer , catalysis , nursing
1 The stereospecificity of the enantiomers of LY253352, a potent and selective α 1 ‐adrenoceptor antagonist, were studied in the human prostate and canine brain using radioligand receptor binding methods. 2 The mean equilibrium dissociation constant ( K D ) in the canine brain and human prostatic adenoma was 84.4 pM and 65.4 pM, respectively. 3 The α 1 ‐adrenoceptor density in the canine brain was approximately eight fold greater than in the human prostatic adenoma. 4 The mean K i values of (−)‐LY253352 and (+)‐LY253352 in the prostate were 0.19 nM and 5.79 nM, respectively. 5 The mean K i values of (−)‐LY253352 and (+)‐LY253352 in the brain were 0.29 nM and 34.7 nM, respectively. 6 This study indicates that the stereochemical specificity of the optical isomers of LY253352 is a manifestation of differential affinities of the enantiomers for α 1 ‐adrenoceptor binding sites. 7 The differential affinities of (+)‐LY253352 in the brain and prostate are suggestive of subtle unique properties of adrenoceptor binding sites in these tissues.