Apamin structure and pharmacology revisited.

ABSTRACT: Apamin is often cited as one of the few substances selectively acting on small-conductance Ca²⁺-activated potassium channels (K_Ca2). However, published pharmacological and structural data remain controversial. Here, we investigated the molecular pharmacology of apamin by two-electrode voltage-clamp in Xenopus laevis oocytes and patch-clamp in HEK293, COS7, and CHO cells expressing the studied ion channels, as well as in isolated rat brain neurons. The microtitre broth dilution method was used for antimicrobial activity screening. The spatial structure of apamin in aqueous solution was determined by NMR spectroscopy. We tested apamin against 42 ion channels (K_Ca, K_V, Na_V, nAChR, ASIC, and others) and confirmed its unique selectiv

SUBMITTER: Kuzmenkov AI 

PROVIDER: S-EPMC9523135 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature