Therapeutic potential of histamine H3 receptor agonists and antagonists. 1998

R Leurs, and P Blandina, and C Tedford, and H Timmerman
Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, Vrije Universiteit, The Netherlands.

The histamine H3 receptor was discovered 15 years ago, and many potent and selective H3 receptor agonists and antagonists have since been developed. Currently, much attention is being focused on the therapeutic potential of H3 receptor ligands. In this review, Rob Leurs, Patrizio Blandina, Clark Tedford and Henk Timmerman describe the available H3 receptor agonists and antagonists and their effects in a variety of pharmacological models in vitro and in vivo. The possible therapeutic applications of the various compounds are discussed.

UI MeSH Term Description Entries
D009435 Synaptic Transmission The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES. Neural Transmission,Neurotransmission,Transmission, Neural,Transmission, Synaptic
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D003071 Cognition Intellectual or mental process whereby an organism obtains knowledge. Cognitive Function,Cognitions,Cognitive Functions,Function, Cognitive,Functions, Cognitive
D004827 Epilepsy A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313) Aura,Awakening Epilepsy,Seizure Disorder,Epilepsy, Cryptogenic,Auras,Cryptogenic Epilepsies,Cryptogenic Epilepsy,Epilepsies,Epilepsies, Cryptogenic,Epilepsy, Awakening,Seizure Disorders
D006633 Histamine Antagonists Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only. Antihistamine,Antihistamines,Histamine Antagonist,Antagonist, Histamine,Antagonists, Histamine
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001289 Attention Deficit Disorder with Hyperactivity A behavior disorder originating in childhood in which the essential features are signs of developmentally inappropriate inattention, impulsivity, and hyperactivity. Although most individuals have symptoms of both inattention and hyperactivity-impulsivity, one or the other pattern may be predominant. The disorder is more frequent in males than females. Onset is in childhood. Symptoms often attenuate during late adolescence although a minority experience the full complement of symptoms into mid-adulthood. (From DSM-V) ADHD,Attention Deficit Disorder,Attention Deficit Hyperactivity Disorder,Brain Dysfunction, Minimal,Hyperkinetic Syndrome,Minimal Brain Dysfunction,ADDH,Attention Deficit Disorders with Hyperactivity,Attention Deficit Hyperactivity Disorders,Attention Deficit-Hyperactivity Disorder,Attention Deficit Disorders,Attention Deficit-Hyperactivity Disorders,Deficit Disorder, Attention,Deficit Disorders, Attention,Deficit-Hyperactivity Disorder, Attention,Deficit-Hyperactivity Disorders, Attention,Disorder, Attention Deficit,Disorder, Attention Deficit-Hyperactivity,Disorders, Attention Deficit,Disorders, Attention Deficit-Hyperactivity,Dysfunction, Minimal Brain,Syndromes, Hyperkinetic
D012890 Sleep A readily reversible suspension of sensorimotor interaction with the environment, usually associated with recumbency and immobility. Sleep Habits,Sleeping Habit,Sleeping Habits,Habit, Sleep,Habit, Sleeping,Habits, Sleep,Habits, Sleeping,Sleep Habit
D017442 Histamine Agonists Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically. Histamine H1 Agonists,Histamine H2 Agonists,Histamine H3 Agonists,H1 Agonist,H1 Agonists,H2 Agonist,H2 Agonists,H3 Agonist,H3 Agonists,Histamine Agonist,Histamine H1 Agonist,Histamine H1 Receptor Agonist,Histamine H1 Receptor Agonists,Histamine H2 Agonist,Histamine H2 Receptor Agonist,Histamine H2 Receptor Agonists,Histamine H3 Agonist,Histamine H3 Receptor Agonists,Histaminergic Agonist,Histaminergic Agonists,Agonist, H1,Agonist, H2,Agonist, H3,Agonist, Histamine,Agonist, Histamine H1,Agonist, Histamine H2,Agonist, Histamine H3,Agonist, Histaminergic,Agonists, H1,Agonists, H2,Agonists, H3,Agonists, Histamine,Agonists, Histamine H1,Agonists, Histamine H2,Agonists, Histamine H3,Agonists, Histaminergic,H1 Agonist, Histamine,H1 Agonists, Histamine,H2 Agonist, Histamine,H2 Agonists, Histamine,H3 Agonist, Histamine,H3 Agonists, Histamine

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