TY - JOUR
T1 - High potent and selective arylpiperazine derivatives as ligands for the 5-HT(1A) receptor
AU - Modica, Maria
AU - Santagati, Maria
AU - Santagati, Andrea
AU - Russo, Filippo
AU - Cagnotto, Alfredo
AU - Goegan, Mara
AU - Mennini, Tiziana
PY - 2000/5/15
Y1 - 2000/5/15
N2 - 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). (C) 2000 Elsevier Science Ltd. All rights reserved.
AB - 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). (C) 2000 Elsevier Science Ltd. All rights reserved.
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U2 - 10.1016/S0960-894X(00)00165-7
DO - 10.1016/S0960-894X(00)00165-7
M3 - Article
C2 - 10843224
AN - SCOPUS:0034658142
VL - 10
SP - 1089
EP - 1092
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 10
ER -