Inhibition of Histamine Synthesis in Brain by α‐Fluoromethylhistidine, a New Irreversible Inhibitor: In Vitro and In Vivo Studies

doi:10.1111/j.1471-4159.1980.tb07858.x

Paper

Inhibition of Histamine Synthesis in Brain by α‐Fluoromethylhistidine, a New Irreversible Inhibitor: In Vitro and In Vivo Studies

Published Nov 1, 1980 · M. Garbarg, G. Barbin, E. Rodergas

Journal of Neurochemistry

Q1 SJR score

236

Citations

6

Influential Citations

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Abstract

a‐Fluoromethylhistidine (α‐FMH), a new potent inhibitor of histidine decarboxylase (HD), has been used for in vitro and in vivo studies of brain HD. Following a preincubation with (+)‐α‐FMH, brain HD activity was inhibited in a time‐dependent and concentration‐dependent manner. The enzyme activity was not restored by overnight dialysis against standard buffer. The (–) antimer of α‐FMH was ineffective. When injected intraperitoneally in a single dose of 20 mg/kg, (±)‐α‐FMH induced a complete loss in HD activity in cerebral cortex and hypothalamus as well as in peripheral tissues, such as stomach. At a dosage of 100 mg/kg (±)‐α‐FMH did not alter histamine‐N‐methyltransferase, DOPA decarboxylase, and glutamate decarboxylase activities. The maximal decrease of HD activity occurred after 2 h in both cerebral cortex and hypothalamus, but the time course of the recovery of enzyme activity was slower in the cerebral cortex. The enzyme activity reached control value within 3 days in hypothalamus and was not fully restored after 4 days in cerebral cortex. Contrasting with the diminished HD activity, a substantial concentration of histamine remained present in five regions of mouse brain. Thus, α‐FMH is a highly specific irreversible inhibitor of brain HD activity and its efficacy makes it useful to study the physiological role of brain histamine.

Non-RCT

Animal Study

Highly Cited

Study Snapshot

a-Fluoromethylhistidine (FMH) is a highly specific and irreversible inhibitor of brain histidine decarboxylase activity, making it useful for studying the physiological role of brain histamine.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Inhibition of Histamine Synthesis in Brain by α‐Fluoromethylhistidine, a New Irreversible Inhibitor: In Vitro and In Vivo Studies

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References

POST MORTEM STABILITY AND STORAGE IN THE COLD OF BRAIN ENZYMES

Post-mortem storage of brain enzymes at 35°C or 70°C for up to 3 months shows stable enzyme activity, while storage at 4°C leads to rapid enzyme decrease.

Selective inhibitors of biosynthesis of aminergic neurotransmitters

Selective inhibitors of key enzymes in neurophysiology and medicine could help understand and correct pathological levels of aminergic neurotransmitters.

Turnover of cerebral histamine in a stressful situation

Stressful situations inhibit the activity of the histaminergic ascending tract to the telencephalon, potentially affecting corticosterone secretion.

Rapid axonal transport of tyrosine hydroxylase in rabbit sciatic nerves

Tyrosine hydroxylase and dopamine--hydroxylase show similar axonal transport velocities in rabbit sciatic nerves, with tyrosine hydroxylase transporting at 0.78 mm/h and dopamine--hydroxylase at 2.4 mm/h.

Dual localization of histamine in an ascending neuronal pathway and in non-neuronal cells evidenced by lesions in the lateral hypothalamic area

Lesions in the lateral hypothalamic area suggest a pluricompartmentation of brain histamine, with histamine localized in an ascending neuronal pathway and in non-neuronal cells, potentially related to nerve impulse flow.

Citations

An In Vivo Definition of Brain Histamine Dynamics Reveals Critical Neuromodulatory Roles for This Elusive Messenger

Histamine release in the brain is sensitive to pharmacological manipulation, with female mice showing more tightly regulated release and antihistamines affecting serotonin levels.

Relationship between Seasonal Changes in Food Intake and Energy Metabolism, Physical Activity, and Body Composition in Young Japanese Women

Seasonal changes in food intake, energy metabolism, and physical activity lead to changes in body composition in young Japanese women.

Targeting Histamine and Histamine Receptors for the Precise Regulation of Feeding.

Histamine plays a complex role in feeding behaviors, including satiety, satiation, motivation, circadian rhythm, and taste perception and memory, making it a potential target for clinical management of obesity and feeding-related disorders.

Inflammation-Induced Histamine Impairs the Capacity of Escitalopram to Increase Hippocampal Extracellular Serotonin

Inflammation-induced histamine impairs the ability of escitalopram to increase extracellular serotonin in the hippocampus, potentially impacting depression treatment.

Role of histamine as a peripheral sympathetic neuromediator and its interrelation with substance P.

Histamine plays a role in regulating peripheral sympathetic reflex through its effect on H3 type receptors, with substance P acting as a sensory neuron mediator.