Results 181 to 190 of about 3,102 (198)

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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Acidic elements in histamine H3 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2010
Antagonists of the human histamine H(3) receptor (hH(3)R) often contain a second basic moiety, which is well known to boost affinity on this histamine receptor subtype. Here, we prepared compounds with acidic moieties of different pK(a) values to figure out that the hH(3)R tolerates these functionalities when added to a common pharmacophore blueprint ...
Kerstin, Sander, Yvonne, von Coburg, Jean-Claude, Camelin, Xavier, Ligneau, Oliver, Rau, Manfred, Schubert-Zsilavecz, Jean-Charles, Schwartz, Holger, Stark   +7 more
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Keynote review: Histamine H3 receptor antagonists reach out for the clinic

Drug Discovery Today, 2005
Antagonists of the histamine H(1) and H(2) receptors have been successful as blockbuster drugs for treating allergic conditions and gastric ulcers, respectively. As such, histamine receptors have made a significant contribution to establishing G-Protein-coupled receptors as the favored drug targets of the industry.
Celanire, S., Wijtmans, M., Talaga, P., Leurs, R., de Esch, I.J.P.   +4 more
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Molecular modeling of histamine H3 receptor and QSAR studies on arylbenzofuran derived H3 antagonists

Journal of Molecular Graphics and Modelling, 2008
Histamine H3 receptors are presynaptic autoreceptors found in both central and peripheral nervous systems of many species. The central effects of these receptors suggest a potential therapeutic role for their antagonists in treatment of several neurological disorders such as epilepsy, schizophrenia, Alzheimer's and Parkinson's diseases.
Siavoush, Dastmalchi, Maryam, Hamzeh-Mivehroud, Taravat, Ghafourian, Hossain, Hamzeiy   +3 more
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Novel human histamine H3 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2002
AbstractFor Abstract see ChemInform Abstract in Full Text.
Chandra, Shah, Laura, McAtee, J Guy, Breitenbucher, Dale, Rudolph, Xiaobing, Li, Timothy W, Lovenberg, Curt, Mazur, Sandy J, Wilson, Nicholas I, Carruthers   +8 more
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Medicinal chemistry of histamine H3 receptor antagonists

1998
Publisher Summary This chapter discusses medicinal chemistry of histamine H3 receptor antagonists and provides an update on the recent progress being made. Several improved clinical candidates have emerged and are progressing towards human clinical trials.
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