Results 171 to 180 of about 6,313 (204)

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
openaire   +2 more sources

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
openaire   +3 more sources

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
openaire   +2 more sources

Design of histamine H3-receptor agonists and antagonists

European Journal of Drug Metabolism and Pharmacokinetics, 1994
The development of highly potent and selective ligands for the characterization of histamine H3-receptors is reviewed. In the field of agonists stereoselectively methylated derivatives of the natural ligand are found to have the desired pharmacodynamic properties. Pharmacokinetic properties could be improved by forming bioreversible azomethine prodrugs
W, Schunack, H, Stark
openaire   +2 more sources

Synthesis of Potent Non-imidazole Histamine H3-Receptor Antagonists

Archiv der Pharmazie, 1998
Histamine has been converted into a non-imidazole H3-receptor histamine antagonist by addition of a 4-phenylbutyl group at the N alpha-position followed by removal of the imidazole ring. The resulting compound, N-ethyl-N-(4-phenylbutyl)amine, remarkably has a Ki = 1.3 microM as an H3 antagonist.
C R, Ganellin, F, Leurquin, A, Piripitsi, J M, Arrang, M, Garbarg, X, Ligneau, W, Schunack, J C, Schwartz   +7 more
openaire   +2 more sources

Dual serotonin transporter inhibitor/histamine H3 antagonists: Development of rigidified H3 pharmacophores

Bioorganic & Medicinal Chemistry Letters, 2007
A series of tetrahydroisoquinolines acting as dual serotonin transporter inhibitor/histamine H(3) antagonists is described. The introduction of polar aromatic spacers as part of the histamine H(3) pharmacophore was explored. A convergent synthesis of the final products allowing late stage introduction of the aromatic side chain was developed.
John M, Keith, Ann J, Barbier, Sandy J, Wilson, Kirstin, Miller, Jamin D, Boggs, Ian C, Fraser, Curt, Mazur, Timothy W, Lovenberg, Nicholas I, Carruthers   +8 more
openaire   +2 more sources

Design of Potent Non-Thiourea H3-Receptor Histamine Antagonists

Journal of Medicinal Chemistry, 1995
Starting from thioperamide, the first potent and selective H3-receptor histamine antagonist, analogues have been synthesized and tested in vitro on rat cerebral cortex to explore structure-activity relationships. The aim has been to design potent compounds which do not possess the thiourea group of thioperamide and which may have improved brain ...
C R, Ganellin, S K, Hosseini, Y S, Khalaf, W, Tertiuk, J M, Arrang, M, Garbarg, X, Ligneau, J C, Schwartz   +7 more
openaire   +2 more sources

Synthesis and SAR of novel histamine H3 receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2006
The synthesis and biological evaluation of novel tetrahydroisoquinoline, tetrahydroquinoline, and tetrahydroazepine antagonists of the human and rat H(3) receptors are described. The substitution around these rings as well as the nature of the substituent on nitrogen is explored.
Cynthia D, Jesudason, Lisa S, Beavers, Jeffrey W, Cramer, Joelle, Dill, Don R, Finley, Craig W, Lindsley, F Craig, Stevens, Robert A, Gadski, Samuel W, Oldham, R Todd, Pickard, Christopher S, Siedem, Dana K, Sindelar, Ajay, Singh, Brian M, Watson, Philip A, Hipskind   +14 more
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Homologs of Histamine as Histamine H3 Receptor Antagonists: A New Potent and Selective H3 Antagonist, 4(5)-(5-Aminopentyl)-1H-imidazole

Journal of Medicinal Chemistry, 1995
The influence of alkyl chain length variation on the histamine H3 receptor activity of histamine homologs 1 was investigated. A series of 4(5)-(omega-aminoalkyl)-1H-imidazoles 1 was prepared with an alkyl chain length varying from one methylene group to 10 methylene groups.
R C, Vollinga, W M, Menge, R, Leurs, H, Timmerman   +3 more
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Acylated and alkylated histamine derivatives as new histamine H3-receptor antagonists

European Journal of Medicinal Chemistry, 1994
New histamine H3-receptor antagonists were prepared and investigated for their ability to increase synthesis and release of histamine mediated by inhibition of presynaptically located H3-receptors. Acyl derivatives of histamine methylated at different positions show poor activity at H3-receptors, whereas Nα-alkyl and particularly Nα-acyl derivatives of
H Stark, R Lipp, JM Arrang, M Garbarg, JC Schwartz, W Schunack   +5 more
openaire   +1 more source