Thioperamide-elicited increase of histamine release from basolateral amygdala of freely moving rats and its therapeutic implications

Cenni, Gabriele; Cangioli, J; Yamatodani, A.; Passani, Maria Beatrice; Mannaioni, P. F.; Felice, A M Di; Blandina, Patrizio

doi:10.1007/s00011-003-0325-2

Cited by 12 publications

(6 citation statements)

References 7 publications

(11 reference statements)

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“…In addition, several selective H 3 antagonist have been shown to increase extracellular histamine levels in the rat prefrontal cortex, the TMN, and the basolateral amygdala after systemic thioperamide administration (Cenni et al, 2004). Together, these studies demonstrate that systemic administration of an H 3 antagonist enhances histaminergic neurotransmission in the CNS.…”

Section: H 3 Receptor Modulation Of Neurotransmitter Releasementioning

confidence: 67%

Discovery of Histamine H₃ Antagonists for the Treatment of Cognitive Disorders and Alzheimer's Disease

Brioni

Esbenshade²,

Garrison³

et al. 2010

J Pharmacol Exp Ther

191

132

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Section: H 3 Receptor Modulation Of Neurotransmitter Releasementioning

confidence: 67%

Discovery of Histamine H₃ Antagonists for the Treatment of Cognitive Disorders and Alzheimer's Disease

Brioni

Esbenshade²,

Garrison³

et al. 2010

J Pharmacol Exp Ther

191

132

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“…These drugs presumably impact on inhibitory H 3 -autoreceptors, as BLA H 3 R receptor binding was strictly associated with the presence of histaminergic fibers [87]. Consistently, BLA perfusion with H 3 R antagonists/inverse agonists increased endogenous histamine release [88], which, in turn, activated postsynaptic H 3 Rs and inhibited ACh release [85]. The BLA receives the most abundant histaminergic innervation in the brain [89], and displays both high H 3 R binding and its gene transcripts [90].…”

Section: Characteristics Of the H 3 Rmentioning

confidence: 74%

Histamine neuronal system as a therapeutic target for the treatment of cognitive disorders

Blandina¹,

Munari

Giannoni

et al. 2010

Future Neurol.

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Much has been learned over the past 20 years about the role of histamine as a neurotransmitter. This brief article attempts to evaluate the progress accomplished in this field, and discusses the therapeutic potential of the H3 receptor (H3R). All histaminergic neurons are localized in the tuberomammillary nucleus of the posterior hypothalamus and project to almost all regions of the CNS. Histamine exerts its effect via interaction with specific receptors (H1R, H2R, H3R and H4R). Antagonists of both H1R and H2R have been successful as blockbuster drugs for treating allergic conditions and gastric ulcers. H4R is still awaiting better functional characterization, but the H3R is an attractive target for potential therapies of CNS disorders. Indeed, considerable interest was raised by reports that pharmacological blockade of H3Rs exerted procognitive effects in a variety of animal tasks analyzing different types of memory. In addition, blockade of H3Rs increased wakefulness and reduced bodyweight in animal models. Such findings hint at the potential use of H3R antagonists/inverse agonists for the treatment of Alzheimer’s disease and other dementias, attention-deficit hyperactivity disorder, obesity and sleep disorders. As a result, an increasing number of H3R antagonists/inverse agonists progress through the clinic for the treatment of a variety of conditions, including attention-deficit hyperactivity disorder, cognitive disorders, narcolepsy and schizophrenia. Moreover, the use of H3R antagonists/inverse agonists that weaken traumatic memories may alleviate disorders such as post-traumatic stress syndrome, panic attacks, specific phobias and generalized anxiety. The use of H3R ligands for the treatment of neurodegenerative disorders is demonstrated in several studies, indicating a role of the histamine neurons and H3Rs in neuroprotection. Recently, direct evidence demonstrated that histaminergic neurons are organized into functionally distinct circuits, impinging on different brain regions, and displaying selective control mechanisms. This could imply independent functions of subsets of histaminergic neurons according to their respective origin and terminal projections. The possibility that H3Rs control only some of those functions implies that H3R-directed therapies may achieve selective effects, with minimal side effects, and this may increase the interest regarding this class of drugs.

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“…In studies using H 1 receptor knockout mice, ciproxifan increased wakefulness only in wild type, yet in both genotypes ciproxifan increased histamine release in the frontal cortex, supporting H 3 receptor antagonist‐evoked histamine release and subsequent H 1 receptor‐mediated vigilance ( Huang et al ., 2006 ). Additionally, evoked histamine release has been demonstrated in the basolateral amygdala following local thioperamide administration ( Cenni et al ., 2004 ). Taken together, these studies suggest that increased release of histamine by H 3 receptor antagonists may act as indirect H 1 and H 2 receptor agonists enhancing histaminergic neurotransmission within the brain with the potential to augment attention in cognitive disorders such as ADHD and AD.…”

Section: H3 Receptor Modulation Of Neurotransmitter Releasementioning

confidence: 99%

The histamine H₃ receptor: an attractive target for the treatment of cognitive disorders

Esbenshade¹,

Browman²,

Bitner³

et al. 2008

British J Pharmacology

276

239

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The histamine H 3 receptor, first described in 1983 as a histamine autoreceptor and later shown to also function as a heteroreceptor that regulates the release of other neurotransmitters, has been the focus of research by numerous laboratories as it represents an attractive drug target for a number of indications including cognition. The purpose of this review is to acquaint the reader with the current understanding of H 3 receptor localization and function as a modulator of neurotransmitter release and its effects on cognitive processes, as well as to provide an update on selected H 3 antagonists in various states of preclinical and clinical advancement. Blockade of centrally localized H 3 receptors by selective H 3 receptor antagonists has been shown to enhance the release of neurotransmitters such as histamine, ACh, dopamine and norepinephrine, among others, which play important roles in cognitive processes. The cognitive-enhancing effects of H 3 antagonists across multiple cognitive domains in a wide number of preclinical cognition models also bolster confidence in this therapeutic approach for the treatment of attention deficit hyperactivity disorder, Alzheimer's disease and schizophrenia. However, although a number of clinical studies examining the efficacy of H 3 receptor antagonists for a variety of cognitive disorders are currently underway, no clinical proof of concept for an H 3 receptor antagonist has been reported to date. The discovery of effective H 3 antagonists as therapeutic agents for the novel treatment of cognitive disorders will only be accomplished through continued research efforts that further our insights into the functions of the H 3 receptor.

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Thioperamide-elicited increase of histamine release from basolateral amygdala of freely moving rats and its therapeutic implications

Cited by 12 publications

References 7 publications

Discovery of Histamine H₃ Antagonists for the Treatment of Cognitive Disorders and Alzheimer's Disease

Discovery of Histamine H₃ Antagonists for the Treatment of Cognitive Disorders and Alzheimer's Disease

Histamine neuronal system as a therapeutic target for the treatment of cognitive disorders

The histamine H₃ receptor: an attractive target for the treatment of cognitive disorders

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Thioperamide-elicited increase of histamine release from basolateral amygdala of freely moving rats and its therapeutic implications

Cited by 12 publications

References 7 publications

Discovery of Histamine H3 Antagonists for the Treatment of Cognitive Disorders and Alzheimer's Disease

Discovery of Histamine H3 Antagonists for the Treatment of Cognitive Disorders and Alzheimer's Disease

Histamine neuronal system as a therapeutic target for the treatment of cognitive disorders

The histamine H3 receptor: an attractive target for the treatment of cognitive disorders

Contact Info

Product

Resources

About

Discovery of Histamine H₃ Antagonists for the Treatment of Cognitive Disorders and Alzheimer's Disease

Discovery of Histamine H₃ Antagonists for the Treatment of Cognitive Disorders and Alzheimer's Disease

The histamine H₃ receptor: an attractive target for the treatment of cognitive disorders