Key result
Qube automated patch-clamp system demonstrates state- and use-dependent inhibition of Nav1.7.
Why the study?
Standardized screening protocols for Nav1.7 channel using high-throughput automated patch-clamp systems are needed to facilitate drug discovery and characterization.
This article provides detailed protocols for high-throughput automated patch-clamp screening of Nav1.7 channels, facilitating drug discovery efforts.
May accelerate Nav1.7 screening workflows; leaves open clinical translation and validation in cardiovascular models.
This article describes the basic procedure for setting up the screening protocol and recording data for Nav1.7 on a Qube automated patch‐clamp system. Three protocols along with step‐by‐step details are provided. First, we describe a protocol to estimate Vhalf, the voltage at which half of the channels are inactivated, using traditional steady‐state inactivation measurement as well as a new adaptive online estimation. Second, we establish a state‐dependent protocol using adaptive online Vhalf measurement to obtain a concentration response curve (CRC) on known reference blockers. Last, we introduce a use‐dependent protocol. In our hands, the sample reference demonstrated good state‐ and use‐dependent inhibition of Nav1.7. © 2020 by John Wiley & Sons, Inc. Basic Protocol 1: Comparing Vhalf measurements using offline calculation and a new adaptive online estimation Basic Protocol 2: Concentration response experiments using a state‐dependent protocol Basic Protocol 3: Concentration response experiments using a use‐dependent protocol Support Protocol: Cell culture protocol
No takes yet. Share an insight, caveat, or question.
Qian et al. (2020) studied this question. Qube automated patch-clamp system protocols was evaluated on Vhalf estimation and concentration response curves. The Qube automated patch-clamp system successfully demonstrated state- and use-dependent inhibition of Nav1.7 using the described screening protocols.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: