IndraLab

Statements

Ketamine inhibits HCN1. 23 / 23
| 23
reach
"Nonetheless, these data argue strongly that ketamine and propofol inhibit HCN1 containing channels and dendritic I h in cortical neurons to mediate enhanced dendritosomatic synaptic integration."
19158287
reach
"Ketamine has been reported to inhibit HCN1 channels[51] and HCN1 was reported necessary for ketamine to exert antidepressant-like actions in mice[62]."
35768639
reach
"In this latter respect, we found that ketamine mediated inhibition of HCN1 containing channels in cortical pyramidal neurons enhances dendritosomatic synaptic integration, an effect that would support the synaptically mediated slow cortical rhythms that accompany the hypnotic state induced by ketamine XREF_BIBR - XREF_BIBR, XREF_BIBR."
23377220
reach
"The authors suggest that ketamine inhibition of HCN1 shifts cortical neuron electroresponsive properties to contribute to ketamine induced hypnosis."
23377220
reach
"Inhibition of HCN1 channels by ketamine accounts for its antidepressant actions."
25571709
reach
"We suggest that ketamine inhibition of HCN1 shifts cortical neuron electroresponsive properties to contribute to ketamine induced hypnosis."
23377220
reach
"These data indicate that HCN2 homomeric channels are relatively unaffected by ketamine, but HCN1 containing channels are strongly inhibited by ketamine in either homomeric or heteromeric configurations."
19158287
reach
"Thus, ketamine inhibits HCN1 containing channels at clinically relevant concentrations and with a stereoselectivity similar to that observed for its anesthetic actions."
19158287
reach
"Whereas such in vitro results provide a strong correlative argument to implicate NMDA receptors, we find that the same case can be made for HCN1 channels : EC 50 values obtained for ketamine inhibition of HCN1 channels are within a clinically relevant range and HCN1 channels are more potently inhibited by S-(+)-ketamine than racemic ketamine."
19158287
reach
"Ketamine reduces HCN1 activity to elicit antidepressant effects."
27965425
reach
"Here, we show that ketamine is a potent inhibitor of cloned HCN1 containing channels and of I h in cortical pyramidal neurons; concordant with its anesthetic actions, we found that inhibition by ketamine is stereoselective and evident at clinically relevant concentrations."
19158287
reach
"In our earlier work, we made the unexpected observation that ketamine inhibited recombinant HCN1 channels at clinically relevant concentrations via a decrease in maximal current amplitude and a hyperpolarizing shift in the V1/2 of channel activation 4."
23377220
reach
"Importantly, whereas ketamine increased EPSP temporal summation by ~ 28% (from 1.9 +/- 0.2 to 2.5 +/- 0.2, n = 5, p < 0.05) in HCN1 f/f mice, this effect of ketamine was totally eliminated in pyramidal neurons of CaMKCre : HCN1 f/f mice (from 3.1 +/- 0.2 to 3.2 +/- 0.2, n = 5, P> 0.05)."
23377220
reach
"Because ketamine also blocks HCN1 channels and these channels are expressed on pyramidal neuron dendrites where they regulate dendrosomatic charge transfer and temporal synchronization, we examined whether the effects of ketamine are mimicked by an HCN inhibitor."
25128848
reach
"The authors previously showed that HCN1 channels are inhibited by ketamine and demonstrated that global HCN1 knockout mice are twofold less sensitive to hypnotic actions of ketamine."
23377220
reach
"As knowledge of the molecular determinants for ketamine inhibition of HCN1 channels becomes available, it may be possible to develop knock-in mice that express ketamine insensitive mutant HCN1 channels, preferably in more restricted neuronal populations, to even more rigorously define the molecular and neuronal targets for this specific clinical endpoint of ketamine."
23377220
reach
"Ketamine caused subunit specific inhibition of recombinant HCN1 containing channels and neuronal I h at clinically relevant concentrations; the channels were more potently inhibited by S-(+)-ketamine than racemic ketamine, consistent with anesthetic actions of the compounds."
19158287
reach
"Ketamine acts as an NMDA receptor (NMDAR) antagonist and also blocks GABA A receptors as well as HCN1 cation channels."
22123167
reach
"On the contrary, higher doses of Ketamine (50-100mg/kg), inhibits both NMDA receptors and the HCN1 pacemaker channels."
21958867
reach
"Ketamine has been reported to inhibit HCN1 channels [51]."
35768639
reach
"Ketamine inhibits HCN1 mediated I h currents at an EC 50 of 15 muM [XREF_BIBR] while it blocks NMDAR channels at EC 50 of 9 muM [XREF_BIBR]."
26268223
reach
"However, HCN1 channel inhibition by ketamine shares a number of characteristics with that described for propofol, including HCN1 subunit-selectivity, insensitivity to cAMP and higher apparent affinity for shifts in V (1/2) than for suppression of maximal current."
19158287
reach
"We previously showed that HCN1 channels are inhibited by ketamine and demonstrated that global HCN1 knockout mice are two-fold less sensitive to hypnotic actions of ketamine."
23377220