The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders

Passani, Maria Beatrice; Lin, Jian‐Sheng; Hancock, Arthur A.; Crochet, Sylvain; Blandina, Patrizio

doi:10.1016/j.tips.2004.10.003

Cited by 216 publications

(131 citation statements)

References 60 publications

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“…Hrh3 knock-out mice have a net decrease of HA levels in the cortex (Toyota et al, 2002) and show reduced anxiety in an elevated plus maze (Rizk et al, 2004) reminiscent of the spd phenotype. Histamine has been linked previously to several behaviors, including aggression, exploration, and boldness (Lecklin et al, 1998;Yanai et al, 1998;Peitsaro et al, 2003;Passani et al, 2004;Masaki and Yoshimatsu, 2006). Thus, HA may have a role as a general regulator of brain function rather than influencing specific behaviors (Wada et al, 1991).…”

Section: Discussionmentioning

confidence: 99%

Modulation of Fgfr1a Signaling in Zebrafish Reveals a Genetic Basis for the Aggression–Boldness Syndrome

Norton¹,

Stumpenhorst²,

et al. 2011

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Behavioral syndromes are suites of two or more behaviors that correlate across environmental contexts. The aggression-boldness syndrome links aggression, boldness, and exploratory activity in a novel environment. Although aggression-boldness has been described in many animals, the mechanism linking its behavioral components is not known. Here we show that mutation of the gene encoding fibroblast growth factor receptor 1a ( fgfr1a) simultaneously increases aggression, boldness, and exploration in adult zebrafish. We demonstrate that altered Fgf signaling also results in reduced brain histamine levels in mutants. Pharmacological increase of histamine signaling is sufficient to rescue the behavioral phenotype of fgfr1a mutants. Together, we show that a single genetic locus can underlie the aggression-boldness behavioral syndrome. We also identify one of the neurotransmitter pathways that may mediate clustering of these behaviors.

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Section: Discussionmentioning

confidence: 99%

Modulation of Fgfr1a Signaling in Zebrafish Reveals a Genetic Basis for the Aggression–Boldness Syndrome

Norton¹,

Stumpenhorst²,

et al. 2011

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“…Noteworthy, BLA perfusion with H 3 -antagonists agonists decreased (Passani et al 2001), whereas with H 3 -agonists increased (Cangioli et al 2002) BLA acetylcholine release, at concentrations comparable to those affecting memory. Inhibitory H 3 -autoreceptors are likely involved, as local perfusion with thioperamide increased BLA histamine release (Cenni et al 2004;Passani et al 2004). Selection of drugs and doses used in the present study stems from those studies, where multiple dosages and several drugs were tested ).…”

Section: Learning and Memory 427mentioning

confidence: 99%

Aversive memory reactivation engages in the amygdala only some neurotransmitters involved in consolidation

Bucherelli¹,

Baldi²,

Mariottini³

et al. 2006

Learn. Mem.

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Consolidation refers to item stabilization in long-term memory. Retrieval renders a consolidated memory sensitive, and a "reconsolidation" process has been hypothesized to keep the original memory persistent. Some authors could not detect this phenomenon. Here we show that retrieved contextual fear memory is vulnerable to amnesic treatments and that the amygdala is critically involved. Cholinergic and histaminergic systems seem to modulate only consolidation, whereas cannabinoids are involved in both consolidation and reactivation. The lability of retrieved memory affords opportunities to treat disorders such as phobias, post-traumatic stress, or chronic pain, and these results help searching for appropriate therapeutic targets.

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“…Brain histamine has several functions including modulation of the neuroendocrine system, 1 drinking behavior, 2 sleep-wake cycles, 3 and feeding behavior. 4 The histamine receptors (H1, H2, H3 and H4) that are known at present are all members of the G-protein-coupled receptor family and they transduce extracellular signals through the G-proteins, Gq, Gs, Gi/o and Gi/o, respectively.…”

Section: Introductionmentioning

confidence: 99%

Effect of histaminergic manipulation on weight in obese adults: a randomized placebo controlled trial

Barak¹,

Greenway

Fujioka

et al. 2008

Int J Obes

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Objective: To determine the magnitude and determinants of weight loss in humans exposed to betahistine, a centrally acting histamine-1 (H-1) agonist and partial histamine-3 (H-3) antagonist. Design: A multicenter randomized, placebo-controlled dose-ranging weight loss trial with a 12-week treatment period. Subjects: Two hundred and eighty-one obese but otherwise healthy participants. Measurements: Weight and obesity-related comorbidities at baseline and at the end of the intervention. Results: Betahistine, at the doses tested, did not induce significant weight loss. With the exception of headache, no difference in adverse effect profile was noted between placebo and treatment groups. Subgroup analysis revealed that age below 50 years, ethnicity (non-Hispanics) and gender (women) were the strongest predictors of weight loss in this population. When these three factors were combined together, the betahistine 48 mg group (n ¼ 23) lost À4.24 ± 3.87 kg, whereas the placebo group (n ¼ 25) lost À1.65±2.96 kg during this time period (P ¼ 0.005). Conclusion: Betahistine, at the doses tested, induced significant weight loss with minimal adverse events only in women below 50 years.

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The histamine H3 receptor as a novel therapeutic target for cognitive and sleep disorders

Cited by 216 publications

References 60 publications

Modulation of Fgfr1a Signaling in Zebrafish Reveals a Genetic Basis for the Aggression–Boldness Syndrome

Modulation of Fgfr1a Signaling in Zebrafish Reveals a Genetic Basis for the Aggression–Boldness Syndrome

Aversive memory reactivation engages in the amygdala only some neurotransmitters involved in consolidation

Effect of histaminergic manipulation on weight in obese adults: a randomized placebo controlled trial

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