Synthesis and In vitro binding affinities of 1-azabicyclic compounds as muscarinic ligands.
Two series of compounds, 2 and 3, were synthesized and their binding affinities were evaluated for the human recombinant muscarinic M(1) receptor subtype expressed in CHO cells. Comparing their binding affinities for the NMS binding sites and the Oxo-M binding sites, they were assumed as agonists. In particular, compound 2e was a good ligand for the agonist binding sites with an IC(50) of 23 nM, which represents over 1585 times stronger binding than for the antagonist binding sites.
Cha
J H
JH
School of Chemistry and Molecular Engineering, Seoul National University, Seoul 151-742, South Korea.
Cho
Y S
YS
Pae
A N
AN
Koh
H Y
HY
Jeong
D
D
Kong
J Y
JY
Lee
E
E
Choi
K I
KI
D000818:Animals; D001372:Aza Compounds / Q000138:chemical synthesis* / Q000378:metabolism*; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis* / Q000378:metabolism*; D016466:CHO Cells; D006224:Cricetinae; D008024:Ligands; D043643:Receptor, Muscarinic M1; D011976:Receptors, Muscarinic / Q000378:metabolism*
D001372:Aza Compounds; D001643:Bridged Bicyclo Compounds; D008024:Ligands; D043643:Receptor, Muscarinic M1; D011976:Receptors, Muscarinic