Tertiapin

Tertiapin

Control of the Upper Airway during Sleep

Published in Susmita Chowdhuri, M Safwan Badr, James A Rowley, Control of Breathing during Sleep, 2022

Recent experiments in rats implicate ACh cells with axonal projections to the XII nucleus in active suppression of activity in XII motoneurons during REM sleep. Specifically, microperfusion of the XII nucleus region with Tertiapin-Q, a blocker of certain K+ channels, increased tongue EMG in a similar pattern to that obtained with perfusion of the XII nucleus with the muscarinic (M) cholinergic receptor antagonist, scopolamine (175). Scopolamine is a broad-spectrum M receptor antagonist; based on the distribution of different M receptors in the brainstem, it was proposed that scopolamine enhanced tongue EMG due to its antagonistic action on M2 receptors (175, 176).

New methodological approaches to atrial fibrillation drug discovery

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Journal Information

Published in Expert Opinion on Drug Discovery, 2021

Chun-Ka Wong, Hung-Fat Tse

The acetylcholine-activated inward rectifying potassiun current (IKACh) is predominantly expressed in the atrium and another potential drug target. In animal studies, IKACh inhibitors such as tertiapin [22] and NTC-801 [23] demonstrated anti-AF activity without prolonging QTc. Nonetheless, these favorable results in animal studies have not been translated into successful clinical trials. Another selective IKACh inhibitor BMS 914,932 failed to reduce AF burden in patients with pacemaker monitoring. Development of another agent, NTC-801, was discontinued in 2013. [23]

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Control of the Upper Airway during Sleep

New methodological approaches to atrial fibrillation drug discovery