Histamine and histamine receptors in Tourette syndrome and other neuropsychiatric conditions

  title={Histamine and histamine receptors in Tourette syndrome and other neuropsychiatric conditions},
  author={Maximiliano Rapanelli and Christopher Pittenger},

Tables from this paper

Histaminergic modulation in Tourette syndrome
A systematic literature review focusing on the role of histaminergic neurotransmission and its pharmacological modulation in Tourette syndrome identified a number of relevant original studies published over the last five years, mainly focusing on genetic aspects.
Histamine H3R receptor activation in the dorsal striatum triggers stereotypies in a mouse model of tic disorders
A novel chemogenetic strategy is used to demonstrate that this dorsal striatal activity is necessary and sufficient for the development of stereotypy: when RAMH-activated cells in the dorsal striatum were chemogenetically activated, stereotypy was recapitulated in KO animals, and when they were silenced the ability of RAMH to produce stereotyping was blocked.
Role of Neuroinflammation in Autism Spectrum Disorder and the Emergence of Brain Histaminergic System. Lessons Also for BPSD?
The hypothesis that central histamine (HA) plays a significant role in the regulation of neuroinflammatory processes of microglia functions in numerous neuropsychiatric diseases, i.e., ASD, AD, SCH, Schizophrenia, epilepsy, and BPSD is examined.
The magnificent two: histamine and the H3 receptor as key modulators of striatal circuitry
  • M. Rapanelli
  • Biology, Psychology
    Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 2017
Histamine modulation of the basal ganglia circuitry in the development of pathological grooming
It is shown that repetitive behavioral pathology in mice derives from deficiency of neurotransmitter HA (rather than HA from other sources), acting in the dorsal striatum, providing a functional dissection of acute HA modulation in the brain and elucidate the anatomical correlates of pathological dysregulation when neuronal HA is disrupted.
Novel Tetrahydroquinazolinamines as Selective Histamine 3 Receptor Antagonists for the Treatment of Obesity.
Therapeutic potential of 4c as an anti-obesity candidate drug via antagonizing the H3R is revealed, and in vitro and docking studies suggested that the 4-methoxy-phenyl-substituted tetrahydroquinazolinamine compound 4c has potent and selective H 3R antagonist activity.
Histidine Decarboxylase Knockout Mice as a Model of the Pathophysiology of Tourette Syndrome and Related Conditions.
  • C. Pittenger
  • Biology
    Handbook of experimental pharmacology
  • 2017
The development and validation of the Hdc-KO model is summarized, which serves as a unique platform to probe the pathophysiology of TS and related conditions, and to generate specific hypotheses for subsequent testing in humans.
Altered expression of histamine signaling genes in autism spectrum disorder
Genome-wide expression and focused gene set analysis in postmortem dorsolateral prefrontal cortex of key HS genes suggest that the HS may be altered in autism spectrum disorder (ASD).


The human histaminergic system in neuropsychiatric disorders
The histamine H3 receptor: an attractive target for the treatment of cognitive disorders
The purpose of this review is to acquaint the reader with the current understanding of H3 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 H3 antagonists in various states of preclinical and clinical advancement.
Histamine H3 antagonists as wake-promoting and pro-cognitive agents.
Recent efforts towards the identification and pharmacological characterization of novel histamine H3 antagonists will be discussed.
Randomized Clinical Study of a Histamine H3 Receptor Antagonist for the Treatment of Adults with Attention-Deficit Hyperactivity Disorder
Bavisant is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.
Interactions of the histamine and hypocretin systems in CNS disorders
The role of the histamine and hypocretin systems in sleep–wake modulation is reviewed and the possibility that narcolepsy-associated histamine abnormalities could mediate or result from the same processes that cause the hypocrretin cell loss is discussed.
Recent advances in histamine H3 receptor antagonists/inverse agonists
Several H3R antagonists/inverse agonists appear to be promising drug candidates, including at least 15 compounds undergoing evaluation in clinical development, especially interesting is pitolisant, which is progressing through to Phase III clinical trials.
Protective effects of histamine H3-receptor ligands in schizophrenic behaviors in experimental models.
Histamine H3 receptor antagonists/inverse agonists on cognitive and motor processes: relevance to Alzheimer's disease, ADHD, schizophrenia, and drug abuse
Whether the H3R inverse agonism modulates the neurochemical basis underlying the disease condition or affects only the cognitive/motor component of the disease process is discussed with the aim to provide a rationale for their use in diverse disease states that are interlinked and are accompanied by some common motor, cognitive and attentional deficits.
Support of the histaminergic hypothesis in Tourette Syndrome: association of the histamine decarboxylase gene in a large sample of families
The results provide strong support for the histaminergic hypothesis in TS etiology and point to a possible role of histamine pathways in neuronal development.
The histaminergic network in the brain: basic organization and role in disease
This Review explores the possible roles of brain histamine in the mechanisms underlying multiple sclerosis and experimental autoimmune encephalitis.