Novel Tetrahydropyridinyl ethylamine and Piperidinyl ethylamine derivatives
- Novel Tetrahydropyridinyl ethylamine and Piperidinyl ethylamine derivatives; their synthesis and biological activities as T-type calcium channel blocker
- their synthesis and biological activities as T-type calcium channel blocker
- 이주현; 강순방; 정낙철; 김유승; 금교창
- Issue Date
- 대한화학회 춘계 학술대회
- VOL 107, P-284
- 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.
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