Novel Tetrahydropyridinyl ethylamine and Piperidinyl ethylamine derivatives

Title
Novel Tetrahydropyridinyl ethylamine and Piperidinyl ethylamine derivatives; their synthesis and biological activities as T-type calcium channel blocker

Title
their synthesis and biological activities as T-type calcium channel blocker
Authors
이주현강순방정낙철김유승금교창
Issue Date
2011-04
Publisher
대한화학회 춘계 학술대회
Citation
VOL 107, P-284
Abstract
T-type Ca2+channel plays important role in modulating neuronal excitability on the central and peripheral neuron system, and is the essential intermediary of hormon secrection. However, hyperactivity of T-type calcium channel generate neurological disorders such as epilepsy, hypertension and neuropathic pain. On the continuous efforts on the development of T-type Ca2+channel blockers. We tried to study on the new drug active on T-type Ca2+ channel with good selectivity as a neuropathic pain therapy. A series of novel Tetrahydropyridinyl ethylamine and Piperidinyl ethylamine derivatives were designed and synthesized based on the 3D pharmacophore model derived from known T-type Ca2+channel blockers. The compounds were studied for the evaluation of in-vitro inhibitory activities with α1G and α1H T-type Ca2+ channel in FDSS assay system, and the selectivity against hERG channel, N-type, and L-type Ca2+channel. Some selected compounds were further studies PK and in-vivo activity using animal model. Therefore, we'll discuss the structure-activity relationship.
URI
http://pubs.kist.re.kr/handle/201004/42766
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KIST Publication > Conference Paper
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