Anaesthetic properties of phencyclidine (PCP) and analogues may be related to their interaction with Na+ channels

Allaoua, Horia; Chicheportiche, Robert

doi:10.1016/0014-2999(89)90202-1

Cited by 28 publications

(11 citation statements)

References 24 publications

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“…13 Increased release of ␤-endorphin could contribute to the analgesic properties of ketamine. Clinically, ketamine increased plasma levels of ␤-endorphin 14 and had long-lasting beneficial effects on postoper- ative pain 15,16 consistent with preemptive analgesia.…”

Section: Discussionmentioning

confidence: 99%

Ketamine stimulates secretion of β-endorphin from a mouse pituitary cell line

YaDeau

Morelli

Billingsley

2003

Regional Anesthesia and Pain Medicine

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Section: Discussionmentioning

confidence: 99%

Ketamine stimulates secretion of β-endorphin from a mouse pituitary cell line

YaDeau

Morelli

Billingsley

2003

Regional Anesthesia and Pain Medicine

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“…It is possible, of course, that differences in species and age may also contribute to the observed differences. The neuroprotective effect of MK-801 in immature animals has, up to this point, been tested 35 Anesthesia may markedly alter the effects of MK-801. 36 Thus, different protocols for anesthetic use may in part explain the differences noted between our results and those of others.…”

Section: Discussionmentioning

confidence: 99%

MK-801 does not protect against hypoxic-ischemic brain injury in piglets.

LeBlanc

Vig

Smith

et al. 1991

Stroke

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Background and Purpose:The excitatory amino acid inhibitor MK-801 has been shown in many animals species to protect against hypoxic-ischemic brain injury. We sought to determine whether hypoxic-ischemic injury to the newborn pig's brain could be prevented by the use of MK-801.Methods: Hypoxic-ischemic injury to the brain was induced in forty 0-3-day-old piglets. They were randomized to receive either 3 mg/kg MK-801 (MK-801 group, n=20) or vehicle (control group, n=19) prior to insult At time 0, the carotid arteries were ligated and the blood pressure was reduced by one third by hemorrhage. At 15 minutes, inspired oxygen was reduced from 50% to 6%. At 30 minutes, inspired oxygen was changed to 100%, carotid ligatures were released, and the withdrawn blood was reinfused. An additional 14 piglets received 3 mg/kg MK-801 but not hypoxic-ischemic injury (drug-only group), and a final group of 11 piglets were subjected to only a sham operation (sham group).Results: Neurological examination scores at 24, 48, and 72 hours showed that MK-801 and drug-only piglets were significantly worse than the controls. Pathological examination of the brains at 72 hours showed significantly greater damage in the brains of the MK-801 and control pigs relative to the sham and drug-only groups. No differences were found between the control and the MK-801 groups. No differences were found between the sham and drug-only groups.Conclusions: MK-801, at a dose of 3 mg/kg, causes neurological dysfunction in piglets lasting at least 72 hours, but neither causes brain damage nor ameliorates the effects of hypoxicischemic injury to the brain of the newborn pig. (Stroke 1991^22:1270-1275)

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“…For example, ketamine inhibits veratridine stimulation-induced Na + uptake with an IC 50 >200 μM. [57] Ketamine also affects Ca 2+ by inhibiting influx and stimulating efflux via the Ca 2+ ATPase. Perhaps most relevantly, ketamine inhibits hyperpolarization-activated cyclic nucleotide-gated at concentrations in the clinically relevant range, with a concentration of drug producing 50% of maximum effect (EC 50 ) of approximately 10 μM.…”

Section: Introduction To Ketaminementioning

confidence: 99%

Ketamine for Treatment-Resistant Unipolar Depression

et al. 2012

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Currently available drugs for unipolar major depressive disorder (MDD), which target monoaminergic systems, have a delayed onset of action and significant limitations in efficacy. Antidepressants with primary pharmacological targets outside the monoamine system may offer the potential for more rapid activity with improved therapeutic benefit. The glutamate system has been scrutinized as a target for antidepressant drug discovery. The purpose of this article is to review emerging literature on the potential rapid-onset antidepressant properties of the glutamate NMDA receptor antagonist ketamine, an established anaesthetic agent. The pharmacology of ketamine and its enantiomer S-ketamine is reviewed, followed by examples of its clinical application in chronic, refractory pain conditions, which are commonly co-morbid with depression. The first generation of studies in patients with treatment-resistant depression (TRD) reported the safety and acute efficacy of a single subanaesthetic dose (0.5 mg/kg) of intravenous ketamine. A second generation of ketamine studies is focused on testing alternate routes of drug delivery, identifying methods to prevent relapse following resolution of depressive symptoms and understanding the neural basis for the putative antidepressant actions of ketamine. In addition to traditional depression rating endpoints, ongoing research is examining the impact of ketamine on neurocognition. Although the first clinical report in MDD was published in 2000, there is a paucity of adequately controlled double-blind trials, and limited clinical experience outside of research settings. Given the potential risks of ketamine, safety considerations will ultimately determine whether this old drug is successfully repositioned as a new therapy for TRD.

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Anaesthetic properties of phencyclidine (PCP) and analogues may be related to their interaction with Na+ channels

Cited by 28 publications

References 24 publications

Ketamine stimulates secretion of β-endorphin from a mouse pituitary cell line

Ketamine stimulates secretion of β-endorphin from a mouse pituitary cell line

MK-801 does not protect against hypoxic-ischemic brain injury in piglets.

Ketamine for Treatment-Resistant Unipolar Depression

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