This paper reports the synthesis and affinities on the 5-HT(1A) versus the α1A receptors of new arylpiperazinylalkylthiothienopyrimidine and thiadiazole derivatives 16-24. Arylpiperazines 16-23 show affinities values in the nanomolar range for the 5-HT(1A) receptor. The compound 16 is highly potent (K(i) 0.26 nM, selectivity 28), the derivatives 20 and 21 are less potent, but highly selective (K(i) 9.40 and 5.06 nM, selectivity 207 and 73, respectively)
High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor
MODICA, Maria Nunziata;SANTAGATI, Andrea;
2000-01-01
Abstract
This paper reports the synthesis and affinities on the 5-HT(1A) versus the α1A receptors of new arylpiperazinylalkylthiothienopyrimidine and thiadiazole derivatives 16-24. Arylpiperazines 16-23 show affinities values in the nanomolar range for the 5-HT(1A) receptor. The compound 16 is highly potent (K(i) 0.26 nM, selectivity 28), the derivatives 20 and 21 are less potent, but highly selective (K(i) 9.40 and 5.06 nM, selectivity 207 and 73, respectively)File in questo prodotto:
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57 2000 Bioorganic & Medicinal Chemistry Letters 10 (2000) 1089-1092.pdf
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