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Literature DB >> 15665857

The histamine H3 receptor: from gene cloning to H3 receptor drugs.

Rob Leurs¹, Remko A Bakker, Henk Timmerman, Iwan J P de Esch.

Abstract

Since the cloning of the histamine H(3) receptor cDNA in 1999 by Lovenberg and co-workers, this histamine receptor has gained the interest of many pharmaceutical companies as a potential drug target for the treatment of various important disorders, including obesity, attention-deficit hyperactivity disorder, Alzheimer's disease, schizophrenia, as well as for myocardial ischaemia, migraine and inflammatory diseases. Here, we discuss relevant information on this target protein and describe the development of various H(3) receptor agonists and antagonists, and their effects in preclinical animal models.

Entities: Disease Gene

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Year: 2005 PMID： 15665857 DOI： 10.1038/nrd1631

Source DB: PubMed Journal: Nat Rev Drug Discov ISSN： 1474-1776 Impact factor: 84.694

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Cited

88 in total

Review 1. Current therapeutic targets for the treatment of Alzheimer's disease.

Authors: Joshua D Grill; Jeffrey L Cummings
Journal: Expert Rev Neurother Date: 2010-05 Impact factor: 4.618

2. The psychostimulant and rewarding effects of cocaine in histidine decarboxylase knockout mice do not support the hypothesis of an inhibitory function of histamine on reward.

Authors: Christian Brabant; Etienne Quertemont; Christelle Anaclet; Jian-Sheng Lin; Hiroshi Ohtsu; Ezio Tirelli
Journal: Psychopharmacology (Berl) Date: 2006-10-28 Impact factor: 4.530

3. Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.

Authors: Xiaofeng Bao; Shuiyu Lu; Jeih-San Liow; Sami S Zoghbi; Kimberly J Jenko; David T Clark; Robert L Gladding; Robert B Innis; Victor W Pike
Journal: J Med Chem Date: 2012-02-16 Impact factor: 7.446

Review 4. Central nervous system biogenic amine targets for control of appetite and energy expenditure.

Authors: David L Nelson; Donald R Gehlert
Journal: Endocrine Date: 2006-02 Impact factor: 3.633

5. Short photoperiod-induced decrease of histamine H3 receptors facilitates activation of hypothalamic neurons in the Siberian hamster.

Authors: P Barrett; M van den Top; D Wilson; J G Mercer; C K Song; T J Bartness; P J Morgan; D Spanswick
Journal: Endocrinology Date: 2009-04-16 Impact factor: 4.736

The histamine H3 receptor: from gene cloning to H3 receptor drugs.

Review 1. Current therapeutic targets for the treatment of Alzheimer's disease.

2. The psychostimulant and rewarding effects of cocaine in histidine decarboxylase knockout mice do not support the hypothesis of an inhibitory function of histamine on reward.

3. Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.

Review 4. Central nervous system biogenic amine targets for control of appetite and energy expenditure.

5. Short photoperiod-induced decrease of histamine H3 receptors facilitates activation of hypothalamic neurons in the Siberian hamster.

6. Marked changes in signal transduction upon heteromerization of dopamine D1 and histamine H3 receptors.

Review 7. Molecular and biochemical pharmacology of the histamine H4 receptor.

8. Interactions between histamine H3 and dopamine D2 receptors and the implications for striatal function.

Review 9. Molecular and cellular analysis of human histamine receptor subtypes.

10. Assessment of the abuse liability of ABT-288, a novel histamine H₃ receptor antagonist.