Synthetic testosterone derivatives modulate rat P2X2 and P2X4 receptor channel gating
نویسندگان
چکیده
منابع مشابه
Comparative Analysis of P2X1, P2X2, P2X3, and P2X4 Receptor Subunits in Rat Nodose Ganglion Neurons
Nodose ganglion (NG) neurons are visceral primary sensory neurons. The transmission and regulation of visceral sensation is mediated mainly by the P2X purinoceptor (P2X receptor). Although the characteristics of different P2X receptor subunits in the NG have been studied previously, comprehensive analyses have not been performed. In this study, we used immunohistochemistry, immunocytochemistry,...
متن کاملVoltage- and [ATP]-dependent Gating of the P2X2 ATP Receptor Channel
P2X receptors are ligand-gated cation channels activated by extracellular adenosine triphosphate (ATP). Nonetheless, P2X(2) channel currents observed during the steady-state after ATP application are known to exhibit voltage dependence; there is a gradual increase in the inward current upon hyperpolarization. We used a Xenopus oocyte expression system and two-electrode voltage clamp to analyze ...
متن کاملRoles of conserved ectodomain cysteines of the rat P2X4 purinoreceptor in agonist binding and channel gating.
Mammalian P2X receptors contain 10 conserved cysteine residues in their ectodomains, which form five disulfide bonds (SS1-5). Here, we analyzed the relevance of these disulfide pairs in rat P2X4 receptor function by replacing one or both cysteines with alanine or threonine, expressing receptors in HEK293 cells and studying their responsiveness to ATP in the absence and presence of ivermectin, a...
متن کاملSecondary Structure and Gating Rearrangements of Transmembrane Segments in Rat P2X4 Receptor Channels
P2X receptors are cation selective channels that are activated by extracellular nucleotides. These channels are likely formed by three identical or related subunits, each having two transmembrane segments (TM1 and TM2). To identify regions that undergo rearrangement during gating and to probe their secondary structure, we performed tryptophan scanning mutagenesis on the two putative TMs of the ...
متن کاملDeciphering the regulation of P2X4 receptor channel gating by ivermectin using Markov models
The P2X4 receptor (P2X4R) is a member of a family of purinergic channels activated by extracellular ATP through three orthosteric binding sites and allosterically regulated by ivermectin (IVM), a broad-spectrum antiparasitic agent. Treatment with IVM increases the efficacy of ATP to activate P2X4R, slows both receptor desensitization during sustained ATP application and receptor deactivation af...
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ژورنال
عنوان ژورنال: Journal of Neurochemistry
سال: 2019
ISSN: 0022-3042,1471-4159
DOI: 10.1111/jnc.14718