Results 181 to 190 of about 6,313 (204)

Non-imidazole histamine H3 ligands. Part III. New 4-n-propylpiperazines as non-imidazole histamine H3-antagonists

European Journal of Medicinal Chemistry, 2005
In search for a new lead of non-imidazole histamine H3-receptor antagonists, a series of 1[(2-thiazolopyridine)-4-n-propyl]piperazines, the analogous 1-[(2-oxazolopyridine)-4-npropyl]piperazines, 1-[(2-benzothiazole)-4-n-propyl]piperazine and 1-[(2-benzooxazole)4-n-propyl]piperazine were prepared and in vitro tested as H3-receptor antagonists (the ...
Krzysztof, Walczyński, Obbe P, Zuiderveld, Henk, Timmerman   +2 more
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Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2010
A series of potent and subtype selective H3 receptor antagonists containing a novel tetrazole core and diamine motif is reported. A one-pot multi-component Ugi reaction was utilised to rapidly develop the structure-activity relationships (SAR) of these compounds. Optimisation for liver microsome stability (t(1/2)>60 min), minimal CYP inhibition (IC(50)>
Adam J, Davenport, Christopher C, Stimson, Massimo, Corsi, Darshan, Vaidya, Edward, Glenn, Timothy D, Jones, Sarah, Bailey, Mark J, Gemkow, Ulrike, Fritz, David J, Hallett   +9 more
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Subclasses of histamine H3 antagonist binding sites in rat brain

Brain Research, 1994
Histamine H3 antagonists have been reported to discriminate subclasses of histamine H3 agonist binding in rat cortical membranes. This phenomenon was investigated by autoradiography of cryostat sections of rat forebrain labelled with [3H]N alpha-methylhistamine ([3H]NAMH, 4 nM). Displacement curves with thioperamide detected a single site in cortex and
Cumming, P, Gjedde, A
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Discovery of novel steroidal histamine H3 receptor antagonists/inverse agonists

Bioorganic & Medicinal Chemistry Letters, 2017
Emerging from an HTS campaign, novel steroid-based histamine H3 receptor antagonists were identified and characterized. Structural moieties of the hit compounds were combined to improve binding affinities which resulted in compound 4 as lead molecule.
Istvan, Ledneczki, Pál, Tapolcsányi, Eszter, Gábor, János, Éles, István, Greiner, Éva, Schmidt, Zsolt, Némethy, Rita Soukupné, Kedves, Ottilia, Balázs, Viktor, Román, György, Lévay, Sándor, Mahó   +11 more
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Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2010
Pre-clinical characterization of novel substituted pyrrolidines that are high affinity histamine H(3) receptor antagonists is described. These compounds efficiently penetrate the CNS and occupy the histamine H(3) receptor in rat brain following oral administration. One compound, (2S,4R)-1-[2-(4-cyclobutyl-[1,4]diazepane-1-carbonyl)-4-(3-fluoro-phenoxy)-
Emily M, Stocking, Leah, Aluisio, John R, Atack, Pascal, Bonaventure, Nicholas I, Carruthers, Christine, Dugovic, Anita, Everson, Ian, Fraser, Xiaohui, Jiang, Perry, Leung, Brian, Lord, Kiev S, Ly, Kirsten L, Morton, Diane, Nepomuceno, Chandravadan R, Shah, Jonathan, Shelton, Akinola, Soyode-Johnson, Michael A, Letavic   +17 more
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Histamine H3 receptor antagonists: From target identification to drug leads

Biochemical Pharmacology, 2007
The successful cloning and functional expression of the histamine H(3) receptor in the late 1990 s has greatly facilitated our efforts to identify small molecule, non-imidazole based compounds to permit the evaluation of H(3) antagonists in models of CNS disorders.
P, Bonaventure, M, Letavic, C, Dugovic, S, Wilson, L, Aluisio, C, Pudiak, B, Lord, C, Mazur, F, Kamme, S, Nishino, N, Carruthers, T, Lovenberg   +11 more
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Therapeutic potential of histamine H3 receptor antagonists in dementias

Drug News & Perspectives, 2010
Selective antagonism of centrally localized histamine H(3) receptors has been shown to enhance the release of a wide spectrum of important neurotransmitters including acetylcholine, gamma-aminobutyric acid, dopamine and noradrenalin, among others, which play fundamental roles in cognitive processes, in an output-dependent manner.
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Potential utility of histamine H3 receptor antagonist pharmacophore in antipsychotics

Bioorganic & Medicinal Chemistry Letters, 2009
Histamine H3 receptor (H3R) antagonists have some antipsychotic properties although the clear molecular mechanism is still unknown. As actually the most effective and less side effective antipsychotics are drugs with multiple targets we have designed typical and atypical neuroleptics with an additional histamine H3 pharmacophore.
Y, von Coburg, T, Kottke, L, Weizel, X, Ligneau, H, Stark   +4 more
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Histamine H3 Antagonists as Wake-Promoting and Pro-Cognitive Agents

Current Topics in Medicinal Chemistry, 2008
The histamine H3 receptor is a pre-synaptic auto- and hetero-receptor that controls the release of histamine and a variety of other neurotransmitters in the brain. As such, modulation of the histamine H(3) receptor is expected to affect wake via control of the release of histamine and to affect cognition via regulation of several other ...
Emily M, Stocking, Michael A, Letavic
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Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors

Bioorganic & Medicinal Chemistry Letters, 2007
A series of novel 4-aryl-1,2,3,4-tetrahydroisoquinoline-based histamine H(3) ligands that also have serotonin reuptake transporter inhibitor activity is described. The synthesis, in vitro biological data, and select pharmacokinetic data for these novel compounds are discussed.
Michael A, Letavic, John M, Keith, Jill A, Jablonowski, Emily M, Stocking, Leslie A, Gomez, Kiev S, Ly, Jennifer M, Miller, Ann J, Barbier, Pascal, Bonaventure, Jamin D, Boggs, Sandy J, Wilson, Kirsten L, Miller, Brian, Lord, Heather M, McAllister, D J, Tognarelli, Jiejun, Wu, Marta C, Abad, Carsten, Schubert, Timothy W, Lovenberg, Nicholas I, Carruthers   +19 more
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