Derivatives of 4-(2'-methoxyphenyl)-1-[2'-(N-2"-pyridinyl-p-iodobenzamido)ethyl]pipera zine (p-MPPI) as 5-HT1A ligands.
A series of new p-alkylbenzamido derivatives of 4-(2'-methoxyphenyl)-1-[2'-(N-2"-pyridinyl)-p- iodobenzamido)ethyl]piperazines (p-MPPI) were prepared. In vitro binding studies suggest that p-methyl and p-ethyl substituents on the benzamido group display the same high binding affinity to 5-HT1A receptors (Ki = 2.2 and 9.3 nM, rat hippocampal homogenates). However, when the substitution groups were larger than a C5 pentyl group, the affinity to 5-HT1A receptors dropped below a useful level (Ki > 50 nM). Several irreversible binding agents (CH2Cl, NHCOCH2Cl) and a photoaffinity labeling compound (m-iodo p-azido) which showed good binding affinity to 5-HT1A receptors were successfully prepared.
Zhuang
Z P
ZP
Department of Radiology, University of Pennsylvania, Philadelphia 19104.
Kung
M P
MP
Chumpradit
S
S
Mu
M
M
Kung
H F
HF
D000345:Affinity Labels / Q000378:metabolism*; D000631:Aminopyridines / Q000378:metabolism*; D000818:Animals; D006624:Hippocampus / Q000378:metabolism; D008024:Ligands; D010879:Piperazines / Q000378:metabolism*; D051381:Rats; D011985:Receptors, Serotonin / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000345:Affinity Labels; D000631:Aminopyridines; D008024:Ligands; D010879:Piperazines; D011985:Receptors, Serotonin; C087205:4-(2'-methoxyphenyl)-1-(2'-(N-(2''-pyridinyl)-4-iodobenzamido)ethyl)piperazine