Results 161 to 170 of about 3,102 (198)

Histamine H₃ Receptor Isoforms: Insights from Alternative Splicing to Functional Complexity. [PDF]

Biomolecules
Gao M, Ooms JF, Leurs R, Vischer HF.
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Non imidazole H3-receptor histamine antagonists

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Deciphering Histamine Pathway Networks in the Human Brain: A Multimodal Approach to Cognition and Psychiatric Disorders

Martins D, Veronese M, Wamelen Dv, Shan L, Howes O, Hampshire A, Turkheimer F, Williams SC.   +7 more
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Novel imidazole-based histamine H3 antagonists

Bioorganic & Medicinal Chemistry Letters, 2009
A novel series of imidazole containing histamine H(3) receptor ligands were investigated and found to be potent functional antagonists. After improving the stability of these molecules towards liver microsomes, these compounds were found to have no appreciable affinity for CYP P450s.
Jill A, Jablonowski, Kiev S, Ly, Michael, Bogenstaetter, Curt A, Dvorak, Jamin D, Boggs, Lisa K, Dvorak, Brian, Lord, Kirsten L, Miller, Curt, Mazur, Sandy J, Wilson, Timothy W, Lovenberg, Nicholas I, Carruthers   +11 more
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Indole- and benzothiophene-based histamine H3 antagonists

Bioorganic & Medicinal Chemistry Letters, 2010
Previous research on histamine H(3) antagonists has led to the development of a pharmacophore model consisting of a central phenyl core flanked by two alkylamine groups. Recent investigation of the replacement of the central phenyl core with heteroaromatic fragments resulted in the preparation of novel 3,5-, 3,6- and 3,7-substituted indole and 3,5 ...
Alejandro, Santillan, Kelly J, McClure, Brett D, Allison, Brian, Lord, Jamin D, Boggs, Kirsten L, Morton, Anita M, Everson, Diane, Nepomuceno, Michael A, Letavic, Alice, Lee-Dutra, Timothy W, Lovenberg, Nicholas I, Carruthers, Cheryl A, Grice   +12 more
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Fluorinated non-imidazole histamine H3 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2009
Fluorine substituents have become a widespread and important component in drug design and development. Here, the synthesis of fluorine containing compounds and some corresponding precursor molecules are presented for potential isotope labelling as well as their data obtained with in vitro and in vivo screenings. The compounds vary in the basic centres (
K, Isensee, M, Amon, A, Garlapati, A, Galaparti, X, Ligneau, J-C, Camelin, M, Capet, J-C, Schwartz, H, Stark   +8 more
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Non-imidazole histamine NO-donor H3-antagonists

Il Farmaco, 2005
Recently a series of H3-antagonists related to Imoproxifan was realised (I); in these products the oxime substructure of the lead was constrained in NO-donor furoxan systems and in the corresponding furazan derivatives. In this paper, a new series of compounds derived from I by substituting the imidazole ring with the ethoxycarbonylpiperazino moiety ...
TOSCO, Paolo, BERTINARIA, Massimo, DI STILO, Antonella, CENA, Clara, FRUTTERO, Roberta, GASCO, Alberto   +5 more
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Influence of histamine H3-antagonists on human leukocytes

Agents and Actions, 1990
To determine the role of the histamine H3-receptor on basophils, different specific H3-antagonists were investigated. Incubation of washed leukocytes with N alpha-acylated histamine-derivatives (N alpha-ahd) induced elevated histamine levels. This process turned out to be dependent on dose, time and temperature, but independent of Ca2+ and Mg2+ ions ...
J, Kleine-Tebbe, J, Schramm, M, Bolz, R, Lipp, W, Schunack, G, Kunkel   +5 more
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Non-Imidazole Histamine H3 Ligands, Part 2: New 2-Substituted Benzothiazoles as Histamine H3 Antagonists

Archiv der Pharmazie, 1999
New, non-imidazole histamine H3 receptor antagonists were prepared and in vitro tested as H3 receptor antagonists measured as the electrically evoked contraction of the guinea-pig jejunum. The 2-(1-piperidinyl)- and 2-(1-pyrrolidinyl)benzothiazoles show no or very poor activity; 2-[1-(4-amino)piperidinyl]- and 2-(1,2-ethanediamino)- and 2-(1,3 ...
Walczynski, K., Guryn, R., Timmerman, H., Zuiderveld, O.P.   +3 more
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Novel H3 receptor antagonists. Sulfonamide homologs of histamine

Bioorganic & Medicinal Chemistry Letters, 1998
Sulfonamides derived from 4(5)-(omega-aminoalkyl)-1H-imidazoles containing chain lengths of three- to five-carbons were synthesized. Good to moderate H3 receptor binding affinities were observed for several butyl and pentyl homologs, whereas binding affinities were considerably weaker in the propyl series.
R, Wolin, M, Connolly, A, Afonso, J A, Hey, H, She, M A, Rivelli, S M, Willams, R E, West   +7 more
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