GABA: 54 (Advances in Pharmacology)

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It is not defined by specific medications or their doses but instead by the patient's response: In pediatric dentistry, N 2 O is an invaluable tool in managing the mildly to moderately anxious child. The ease of its administration, its wide margin of safety, its analgesic and anxiolytic effects, and, most of all, its rapid reversibility make it an ideal drug for use in children.

The mechanisms involved are not yet completely understood. This is also supported by observations that N 2 O-induced depression of visual evoked potentials is antagonized by a benzodiazepine inverse agonist. N 2 O- and benzodiazepine-induced anxiolytic-like effects in animal models of anxiety are also sensitive to antagonism by inhibition of NOS, a family of enzymes responsible for the synthesis of NO.

Studies in the elevated plus maze revealed that the increased open-arm activity produced by N 2 O and chlordiazepoxide was blocked by a nonselective NOS inhibitor; this antagonism was stereoselectively reversed by L-arginine. Mechanism of N 2 O-induced anxiolysis. N 2 O is thought to cause activation of the benzodiazepine BZ binding site as its effects are blocked by flumazenil.

The increased chloride ion concentration in the neuron might cause activation of calmodulin CaM , which then activates the enzyme nitric oxide synthase NOS. In a manner similar to how N 2 O activates opioid receptors, it is plausible that N 2 O may induce neuronal release of endogenous benzodiazepine factors that then stimulate the GABA A receptor. N 2 O has a well-known role in medical history because it was the first drug used for surgical anesthesia.

Despite its limited anesthetic potency, N 2 O is the most widely used general anesthetic agent. But more recently, it has been suggested that general anesthetics might act on one or more superfamilies of ligand-gated ion channels that include GABA A , glycine, nicotinic acetylcholine, 5-hydroxytryptamine 3 , and glutamate receptors. N 2 O itself has been reported to affect various ligandgated ion channels. N-methyl-D-aspartate NMDA -type glutamate receptors have recently emerged as a possible target of inhalation anesthetic drugs.

The 2 drugs, in fact, produce synergistic neurotoxicity when used together. It is apparent from the above discussion that N 2 O has multiple mechanisms of action that underlie its varied pharmacological properties. Current research indicates that the analgesic effect of N 2 O appears to be initiated by stimulated neuronal release of endogenous opioid peptides, with subsequent activation of opioid receptors and descending GABA and noradrenergic pathways that modulate nociceptive processing at the spinal level.

The anxiolytic effect of N 2 O involves activation of the GABA A receptor through the benzodiazepine binding site, although whether N 2 O acts directly or indirectly upon the latter targets remains uncertain. The anxiolytic pathway that is stimulated includes a segment that involves a sequence of 3 key enzymes, NOS, soluble guanylyl cyclase, and PKG. The anesthetic effect of N 2 O appears to be caused by inhibition of NMDA glutamate receptors and removing its excitatory influence in the nervous system.

National Center for Biotechnology Information , U. Journal List Anesth Prog v. Received May 11; Accepted Sep 9. This article has been cited by other articles in PMC. Abstract Nitrous oxide N 2 O has been used for well over years in clinical dentistry for its analgesic and anxiolytic properties. Nitrous oxide, Pharmacology, Anesthesia, Analgesia, Anxiolysis. Involvement of Nitric Oxide in N 2 O Antinociception Nitric oxide NO is a naturally occurring gas that only recently has been recognized as an endogenous biological regulator of great significance.

Open in a separate window. Descending Pathways Activated by N 2 O Fujinaga and Maze 53 hypothesized that the release of endogenous opioid peptides and the subsequent stimulation of opioid receptors activate descending pathways that modulate nociceptive processing in the spinal cord. Tolerance to N 2 O Antinociception As with many centrally mediated drug effects, continuous administration of N 2 O results in development of tolerance to the antinociceptive effect of N 2 O in experimental animals 39 and to the analgesic effect of N 2 O in human subjects.

A consideration of factors in the discovery of anesthesia and their effects on its development. Nitrous oxide in dental practice. Dundee JW, Moore J. Alterations in response to somatic pain associated with anaesthesia. The effect of sub-anaesthetic concentrations of inhalation agents. Nitrous oxide for relief of labor pain. Am J Obstet Gynecol. Self-administered nitrous oxide for the management of incident pain in terminally ill patients: Nitrous oxide analgesia during intra-articular injection for juvenile idiopathic arthritis.

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Inhaled nitrous oxide versus placebo as an analgesic and anxiolytic adjunct to peripheral intravenous cannulation. Am J Emerg Med. The use of inhaled nitrous oxide for flexible sigmoidoscopy: Nitrous oxide for colonoscopy: Entonox as an analgesic agent during panretinal photocoagulation. Nitrous oxide entonox inhalation and tolerance of transrectal ultrasound guided prostate biopsy: Use of Entonox in the ambulance service. Ann Pediatr Paris ; Annequin D, Hamon R. The analgetic effects of low concentrations of nitrous oxide compared in man with morphine sulphate.

J Pharmacol Exp Ther. Nitrous oxide effects on cerebral evoked potential to pain: Paradoxical effect of naloxone on nitrous oxide analgesia in man. Opiate-like analgesic activity in general anaesthetics. Antagonism of nitrous oxide analgesia by naloxone in man. Evaluation of the periaqueductal central gray PAG as a morphine-specific locus of action and examination of morphine-induced and stimulation-produced analgesia at coincident PAG loci. Antagonism of nitrous oxide antinociception in the rat hot plate test by site-specific mu and epsilon opioid receptor blockade.

Opiate receptors in the periaqueductal gray mediate analgesic effect of nitrous oxide in rats. Nitrous oxide N 2 O antinociception in the mouse abdominal constriction test is mediated by opioid receptors in the periaqueductal gray region of the brain. Proc West Pharmacol Soc. Fujinaga M, Maze M. Neurobiology of nitrous oxide-induced antinociceptive effects. Influence of narcotic antagonist drugs upon nitrous oxide analgesia in mice.

Quock RM, Mueller J. Mediation of nitrous oxide analgesia in mice by spinal and supraspinal kappa-opioid receptors. Role of brain dynorphin in nitrous oxide antinociception in mice. Antagonism of nitrous oxide antinociception in mice by intrathecally administered antisera to endogenous opioid peptides. Tolerance to nitrous oxide analgesia in rats and mice.

Does nitrous oxide induce release of brain opioid peptides? The effects of nitrous oxide on the central endogenous pro-opiomelanocortin system in the rat. The effects of nitrous oxide on the secretory activity of pro-opiomelanocortin peptides from basal hypothalamic cells attached to cytodex beads in a superfusion in vitro system. Spinal involvement of both dynorphin A and Met-enkephalin in the antinociception induced by intracerebroventricularly administered bremazocine but not morphine in the mouse.

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Nitric oxide as modulator of neuronal function. Inhibitors of nitric oxide synthesis antagonize nitrous oxide antinociception in mice and rats. Role of nitric-oxide synthase isoforms in nitrous oxide antinociception in mice. Antagonism of nitrous oxide antinociception in mice by antisense oligodeoxynucleo-tide directed against neuronal nitric oxide synthase enzyme.

Strain-dependent differences in responsiveness of mice to nitrous oxide N 2 O antinociception. Nitrous oxide antinociception in BXD recombinant inbred mouse strains and identification of quantitative trait loci. Correlation of inbred mouse sensitivity to nitrous oxide antinociception with brain nitric oxide synthase activity following exposure to nitrous oxide.

Detection and mapping of quantitative trait loci that determine responsiveness of mice to nitrous oxide antinociception. Localization of the neuronal form of nitric oxide synthase to mouse chromosome 5. The analgesic action of nitrous oxide is dependent on the release of norepi-nephrine in the dorsal horn of the spinal cord. Antinociceptive response to nitrous oxide is mediated by supraspinal opiate and spinal alpha 2 adrenergic receptors in the rat.

Advances in Understanding the Actions of Nitrous Oxide

Evidence for the involvement of spinal cord alpha 1 adrenoceptors in nitrous oxide-induced antinociceptive effects in Fischer rats. The functional development of descending inhibitory pathways in the dorsolateral funiculus of the newborn rat spinal cord. Postnatal development of the cutaneous flexor reflex: Dev Med Child Neurol.

Nitrous oxide lacks the antinociceptive effect on the tail flick test in newborn rats. Nitrous oxide exerts age-dependent antinociceptive effects in Fischer rats.


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GABAergic interneurons at supraspinal and spinal levels differentially modulate the antinociceptive effect of nitrous oxide in Fischer rats. Brain stem opioidergic and GABAergic neurons mediate the antinociceptive effect of nitrous oxide in Fischer rats.

ADVANCES IN PHARMACOLOGY, VOLUME 54: GABA

Tolerance to nitrous oxide in volunteers. Strain differences in antinociceptive effect of nitrous oxide on tail flick test in rats.


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    • Dopaminergic reward regions of Lewis and Fischer rats display different levels of tyrosine hydroxylase and other morphine- and cocaine-regulated phosphoproteins. Brain dynorphin and enkephalin systems in Fischer and Lewis rats: The involvement of the central cholinergic and endorphinergic systems in the nitrous oxide withdrawal syndrome in mice.

    Volume 54 of the Advances in Pharmacology series has also provided new insights into fundamental features of neurotransmission in general, such as the importance of allosterism and coincident A great deal of progress has been made in defining GABA gamma-aminobutyric acid transmission in the brain. Volume 54 of the Advances in Pharmacology series has also provided new insights into fundamental features of neurotransmission in general, such as the importance of allosterism and coincident signaling in regulating receptor function and overall cellular activity.

    These studies have led to the design and development of new drugs and potential therapeutic agents.

    Molecular Pharmacology of Neurotransmitter Receptors Advances in Biochemical Psychopharmacology PDF

    Given the successes achieved over the first 50 years of GABA research, it is certain the 6th decade will yield its share of surprising discoveries and new insights. Published in this volume are articles providing thoughts and perspectives on this topic, some with the benefit of hindsight, others in the context of recent findings, but all with a hint, or prediction, of what the future holds as the secrets of GABA neurotransmission continue to unfold.

    Advances in Pharmacology is available online on ScienceDirect - full-text online of volumes 48 onwards. Ferid Murad was born in Whiting, Indiana. Working concurrently on an M. His many honors include the Alfred S.