Chemical and Pharmaceutical Bulletin p. 672 - 677 (1999)
Update date:2022-08-11
Topics:
Watanabe, Toshihiro
Kinoyama, Isao
Takizawa, Kenji
Hirano, Seiko
Shibanuma, Tadao
A series of 1,2,3,4-tetrahydroisoquinoline derivatives containing the 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one skeleton were prepared and evaluated for their in vitro binding affinities to muscarinic receptors and for antagonism of bradycardia in vivo. Among them, compound 3f had the highest affinity for M2 muscarinic receptors in the heart (pKi=9.1) with low affinity for M3 muscarinic receptors in the submandibular gland. A structure-activity relationship (SAR) study suggested that the benzene ring fused piperidine and the alkyl linker chain length are crucially important for increased M2 affinity.
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