Pharmacological Characterization of the Novel Histamine H3-Receptor Antagonist N-(3,5-Dichlorophenyl)-N′-[[4-(1H-imidazol-4-ylmethyl)phenyl]-methyl]-urea (SCH 79687)

No abstract is available for this paper.

• Publication year

  2003

• Venue

  Journal of Pharmacology and Experimental Therapeutics

• Publication date

  2003-06-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1124/JPET.103.049254PMID 12649305
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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  2001cited by this paper
• Intranasal Application of the α2-Adrenoceptor Agonist BHT-920 Produces Decongestion in the Cat

  2001cited by this paper
• The histamine H3 receptor and its ligands.

  2001cited by this paper
• Discovery of a novel member of the histamine receptor family.

  2001cited by this paper
• Histamine H3 receptor-mediated inhibition of sympathetically evoked mydriasis in rats.

  2001cited by this paper
• Species-related pharmacological heterogeneity of histamine H(3) receptors.

  2001cited by this paper
• Cloning and characterization of a novel human histamine receptor.

  2001cited by this paper
• Histamine H3 Antagonists

  2001influential reference
• Cloning of rat histamine H(3) receptor reveals distinct species pharmacological profiles.

  2000cited by this paper
• Antiallergic effects of H1‐receptor antagonists

  2000cited by this paper
• Cognitive, social, and economic costs of allergic rhinitis.

  2000cited by this paper
• Nasal Congestion: A Review of its Etiology, Evaluation, and Treatment

  2000cited by this paper
• Molecular cloning and characterization of a new human histamine receptor, HH4R.

  2000cited by this paper
• Pharmacological characterization of histamine H3 receptors in human saphenous vein and guinea pig ileum.

  1999cited by this paper
• Hyperresponsiveness in the human nasal airway: new targets for the treatment of allergic airway disease.

  1999cited by this paper
• Combined Histamine H1 and H3 Receptor Blockade Produces Nasal Decongestion in an Experimental Model of Nasal Congestion

  1999cited by this paper
• Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice.

  1998influential reference
• Pharmacokinetic screening for the selection of new drug discovery candidates is greatly enhanced through the use of liquid chromatography-atmospheric pressure ionization tandem mass spectrometry.

  1997cited by this paper
• Presynaptic imidazoline receptors and non‐adrenoceptor[3H]‐idazoxan binding sites in human cardiovascular tissues

  1997cited by this paper
• Pharmacological characterization of histamine H3 receptors in isolated guinea pig pulmonary artery and ileum.

  1995cited by this paper
• Molecular pharmacological aspects of histamine receptors.

  1995cited by this paper
• Comparison of the glucose-lowering properties of vanadyl sulfate and bis(maltolato)oxovanadium(IV) following acute and chronic administration.

  1995cited by this paper
• New aspects of the role of histamine in cardiovascular function: identification, characterization, and potential pathophysiological importance of H3 receptors.

  1995cited by this paper
• Mechanisms of rhinitis

  1994cited by this paper
• Binding characteristics of a histamine H3-receptor antagonist, [3H]S-methylthioperamide: comparison with [3H](R)alpha-methylhistamine binding to rat tissues.

  1994cited by this paper
• Production by R‐α‐methylhistamine of a histamine H3 receptor‐mediated decrease in basal vascular resistance in guinea‐pigs

  1993cited by this paper
• Inhibition of sympathetic hypertensive responses in the guinea‐pig by prejunctional histamine H3‐receptors

  1992cited by this paper
• Allergic rhinitis: a review.

  1992cited by this paper
• Activation of histamine H3 receptors produces presynaptic inhibition of neurally evoked cat nictitating membrane responses in vivo

  1992cited by this paper
• Goodman and Gilman's The Pharmacological Basis of Therapeutics

  1991cited by this paper
• Histamine receptors in isolated guinea pig duodenal muscle: H3 receptors inhibit cholinergic neurotransmission.

  1991cited by this paper
• Drug thearapy : allergic rhinitis

  1991cited by this paper
• Inhibition of electrically evoked contractions of guinea-pig ileum preparations mediated by the histamine H3 receptor.

  1990influential reference
• Identification of two H3-histamine receptor subtypes.

  1990cited by this paper
• Alpha‐adrenoceptors: A critical review

  1989influential reference
• Pharmacologic methods for identification of receptors.

  1988influential reference
• Manual of Pharmacologic Calculations: With Computer Programs

  1984cited by this paper
• Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor

  1983cited by this paper
• Manual of Pharmacologic Calculations

  1981cited by this paper
• H-2 histamine receptors.

  1979cited by this paper

• CP-MLR/PLS-guided Quantitative Structure-activity Relationship Study on the Derivatives of Benzimidazolone as H3-Antihistaminic Agents.

  2025cites this paper
• Histamine H3 receptor antagonists - Roles in neurological and endocrine diseases and diabetes mellitus.

  2022cites this paper
• New antihistamines – perspectives in the treatment of some allergic and inflammatory disorders

  2018cites this paper
• Histamine H3R Antagonists: From Scaffold Hopping to Clinical Candidates

  2016cites this paper
• The Histamine H3 Receptor: Structure, Pharmacology, and Function

  2016cites this paper
• Cherry-picked ligands at histamine receptor subtypes.

  2016cites this paper
• Anticonvulsant and Precognitive Properties Of Novel Histamine H3 Receptor Antagonists in Male Adult Rats

  2016cites this paper
• Imetit Dihydrobromide and Thioperamide Medication in Cough Hypersensitivity Model—The Role of H3 Receptors

  2016cites this paper
• International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors

  2015influential citation
• Synthesis and SAR studies of benzimidazolone derivatives as histamine H3-receptor antagonists.

  2013cites this paper
• The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.

  2011cites this paper
• Histamine H3 receptor as a drug discovery target.

  2011cites this paper
• Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764).

  2011cites this paper
• The synthesis and structure-activity relationship of 4-benzimidazolyl-piperidinylcarbonyl-piperidine analogs as histamine H3 antagonists.

  2010cites this paper
• Histamine H3 antagonists as wake-promoting and pro-cognitive agents.

  2008cites this paper
• Drug Discovery: From Hits to Clinical Candidates

  2008cites this paper
• 4-benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists.

  2008cites this paper
• Structurally novel histamine H3 receptor antagonists GSK207040 and GSK334429 improve scopolamine-induced memory impairment and capsaicin-induced secondary allodynia in rats.

  2007cites this paper
• Generation of a homology model of the human histamine H3 receptor for ligand docking and pharmacophore-based screening

  2007cites this paper
• 4-[6-(2-Aminoethyl)naphthalen-2-yl]benzonitriles are potent histamine H3 receptor antagonists with high CNS penetration.

  2007cites this paper
• Histamine H3 receptor ligands break ground in a remarkable plethora of therapeutic areas

  2007cites this paper
• Novel heterocyclic-substituted benzofuran histamine H3 receptor antagonists: in vitro properties, drug-likeness, and behavioral activity.

  2007cites this paper
• 4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists.

  2007cites this paper
• An Expedient and Multikilogram Synthesis of a Naphthalenoid H3 Antagonist

  2007cites this paper
• Synthesis and biological evaluation of new non-imidazole H3-receptor antagonists of the 2-aminobenzimidazole series.

  2006cites this paper
• Recent medicinal chemistry of the histamine H3 receptor.

  2006cites this paper
• Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists.

  2006cites this paper
• An efficient and convergent synthesis of the potent and selective H3 antagonist ABT-239

  2006cites this paper
• Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.

  2006cites this paper
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  2005cites this paper
• The histamine H3 receptor: from gene cloning to H3 receptor drugs

  2005cites this paper
• Roles of histamine and its receptors in allergic and inflammatory bowel diseases.

  2005cites this paper
• Histamine-mediated mechanisms in the human nasal airway.

  2005cites this paper
• Keynote review: histamine H3 receptor antagonists reach out for the clinic.

  2005cites this paper
• Effects of activation of central nervous histamine receptors in cardiovascular regulation; studies in H1 and H2 receptor gene knockout mice

  2005cites this paper
• Histamine receptors that influence blockage of the normal human nasal airway

  2005cites this paper
• A new class of potent non-imidazole H(3) antagonists: 2-aminoethylbenzofurans.

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• Activation of histamine H3 receptors in human nasal mucosa inhibits sympathetic vasoconstriction.

  2004cites this paper
• Medicinal chemistry and biological properties of non-imidazole histamine H3 antagonists.

  2004cites this paper
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  2004cites this paper