100 Most amide- and ester-based local anesthetics are weak bases, and both protonated and unprotonated forms exist in equilibrium at normal pH. While it is the unprotonated form that easily crosses the cell membrane, only the protonated form is able to block Na+ channels. Thus, local ...
TASK-1 (KCNK3) and TASK-3 (KCNK9) subunits are functional when associated as homodimers or heterodimers. TASK channels display strong basal currents with very fast activation and inactivation kinetics. TREK channels, which comprise TREK-1 (KCNK2), TREK-2 (KCNK10), and TRAAK (KCNK4), ...
activated (BK) potassium channels are the SKCachannels' low conductance (less than 50 pS), the weak or negligible dependence of their activity on membrane voltage, and their high affinity for calcium (EC50<1 μM) (e.g., Lancaster, B., and Zucker, R. S.,J. Physiol.475:229–239, ...
KATP channels display weak rectification; however, it has been shown that just a single amino acid substitution in the so-called rectification controller region of inward rectifiers (see Fig. 4.2, Kir2.1; N160D in Kir6.2) converts Kir6.2 into a strongly rectifying channel.53 A defining propert...
TRPV4TRPVKeratinocytes, Merkel cells, Aβ-fibers, C-fibersYesReduced response to strong pressure; no change in C-fiber mechanical threshold after inflammationIncreased response threshold to strong mechanical stimuli; reduced neuropathic mechanical hyperalgesia; reduced inflammatory mechanical hyperalgesia[36,37...
Fig. 2. Mouse (NM_010610, w/o splice exon plus first 27 residues from L16912), rat (NM_031828, w/o splice exons), and human (NM_002247) BK alpha subunits (Slo). (*) single, fully conserved residue; (:) conservation of strong groups, (.) conservation of weak groups, (-) no ...
When the distribution of Kcnk3 message in mouse heart was examined by in situ hybridization, a strong, specific signal was apparent throughout both ventricles with the antisense probe (Fig.2 C). A weak antisense signal was also visualized in the atria, indicating a lower level of transcript ...
A distinguishing feature of TWIK-1 (KCNK1) is its weak inward rectification, which results in significant outward currents between -60 and 0 mV.6279 These channels are activated by PKC and inhibited by intracellular acidification.79 In contrast, TASK-1 (KCNK3) and TRAAK (KCNK4) currents ...
KATP is a receptor-activated weak inward rectifier channel, regulated by intracellular ATP and ADP concentrations. An increase in the ratio of ATP to ADP closes the channel, and a decrease opens it, linking the metabolic state to the cellular Em.16,41-43 Function IKATP is inhibited by intrac...