Synthesis and pharmacological characterization of 2-(4-chloro-3-hydroxyphenyl) ethylamine and N, N-dialkyl derivatives as dopamine receptor ligands

…, G Giorgioni, A Di Stefano, MP Abbracchio…

Index: Claudi, Francesco; Giorgioni, Gianfabio; Stefano, Antonio Di; Abbracchio, Maria Pia; Paoletti, Anna Maria; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 23 p. 4408 - 4414

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Citation Number: 18

Abstract

7c CI,, H of DA receptors of 2-(4-fluoro-3-hydroxyphenyl) ethy-lamine (3) and some NJV- dialkyl derivatives. l4 Amine 3 showed about 2-fold lower affinity than DA for both binding sites, whereas theN-ethyl-N-(2-phenylethyl)(3a) and Nn-propyl-N-(2-phenylethyl)(3b) derivatives had high affmity and selectivity for D-2 binding sites. The behavioral teata on rata indicated that 3b crosses the bloodbrain barrier and exerta an agonistic effect on the ...