H3 antagonist

An H3-receptor antagonist is a classification of drugs used to block the action of histamine on the Histamine H3 receptor. Unlike the H1 and H2 receptors which have primarily peripheral actions, but cause sedation if they are blocked in the brain, H3 receptors are primarily found in the brain and are inhibitory autoreceptors located on histaminergic nerve terminals, which modulate the release of histamine. Histamine release in the brain triggers secondary release of excitatory neurotransmitters such as glutamate and acetylcholine via stimulation of H1 receptors in the cerebral cortex. Consequently unlike the H1 antagonist antihistamines which are sedating, H3 antagonists have stimulant and nootropic effects, and are being researched as potential drugs for the treatment of neurodegenerative conditions such as Alzheimer's disease.

Examples of selective H3 antagonists include clobenpropit,cite journal |author=Yoneyama H, Shimoda A, Araki L, "et al" |title=Efficient approaches to S-alkyl-N-alkylisothioureas: syntheses of histamine H3 antagonist clobenpropit and its analogues |journal=J. Org. Chem. |volume=73 |issue=6 |pages=2096–104 |year=2008 |month=March |pmid=18278935 |doi=10.1021/jo702181x |url=http://dx.doi.org/10.1021/jo702181x] ABT-239,cite journal | author = Fox GB, Esbenshade TA, Pan JB, Radek RJ, Krueger KM, Yao BB, Browman KE, Buckley MJ, Ballard ME, Komater VA, Miner H, Zhang M, Faghih R, Rueter LE, Bitner RS, Drescher KU, Wetter J, Marsh K, Lemaire M, Porsolt RD, Bennani YL, Sullivan JP, Cowart MD, Decker MW, Hancock AA | title = Pharmacological properties of ABT-239 [4-(2-{2- [(2R)-2-Methylpyrrolidinyl] ethyl}-benzofuran-5-yl)benzonitrile] : II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist | journal = J. Pharmacol. Exp. Ther. | volume = 313 | issue = 1 | pages = 176–90 | year = 2005 | pmid = 15608077 | doi = 10.1124/jpet.104.078402 | issn = ] ciproxifan,cite journal | author = LLigneau X, Lin J, Vanni-Mercier G, Jouvet M, Muir JL, Ganellin CR, Stark H, Elz S, Schunack W, Schwartz J | title = Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist | journal = J. Pharmacol. Exp. Ther. | volume = 287 | issue = 2 | pages = 658–66 | year = 1998 | month = November | pmid = 9808693 | doi = 10.1016/j.bcp.2007.01.002 | url = | issn = ] and A-349,821. [Esbenshade TA, Fox GB, Krueger KM, Baranowski JL, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan JB, Faghih R, Bennani YL, Williams M, Hancock AA. Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. "Biochemical Pharmacology". 2004 Sep 1;68(5):933-45. PMID 15294456]

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  • antagonist — ANTAGONÍST, Ă, antagonişti, ste, adj. Care se află în antagonism (unul faţă de altul); antagonic. ♢ Contradicţie antagonistă = contradicţie antagonică. – Din fr. antagoniste, lat. antagonista. Trimis de ana zecheru, 28.02.2009. Sursa: DEX 98 … …   Dicționar Român

  • Antagonist — (griech. ανταγωνιστής, antagonistís, von αντι, anti, „gegen“ und άγω, ágo, „ich handle, bewege, führe“: „der Gegenhandelnde“, „der Gegenspieler“) bezeichnet: im allgemeinen einen Widersacher oder Gegner Antagonist (Literatur), der Gegenspieler… …   Deutsch Wikipedia

  • Antagonist — An*tag o*nist, n. [L. antagonista, Gr. ?; ? against + ? combatant, champion, fr. ?: cf. F. antagoniste. See {Antagonism}.] 1. One who contends with another, especially in combat; an adversary; an opponent. [1913 Webster] Antagonist of Heaven s… …   The Collaborative International Dictionary of English

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  • Antagonist Perpetrated Aggression — Antagonist Perpetrated AggressionAPA , [http://en.wikibooks.org/wiki/Tactical Combat#APA TACTICAL ANTAGONIST PERPETRATED AGGRESSION APA Tactical Combat] Training System is a proven special force response system,… …   Wikipedia

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  • Antagonist — Antagonist, so viel als Gegner, Widersacher, Feind …   Damen Conversations Lexikon

  • antagonist — index adversary, aggressor, assailant, contender, contestant, disputant, foe, rival Burton s Legal Thesaurus …   Law dictionary

  • antagonist — (n.) 1590s, from Fr. antagoniste (16c.) or directly from L.L. antagonista, from Gk. antagonistes competitor, opponent, rival, agent noun from antagonizesthai to struggle against, oppose, be a rival, from anti against (see ANTI (Cf. anti )) +… …   Etymology dictionary

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  • antagonist — *opponent, adversary Analogous words: foe, *enemy: rival, competitor (see corresponding verbs at RIVAL): assailant, attacker (see corresponding verbs at ATTACK) Antonyms: supporter Contrasted words: ally, *partner, colleague …   New Dictionary of Synonyms


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