Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Helmut Ensinger"'
Publikováno v:
Arzneimittelforschung. 51:947-954
The pharmacokinetics of 1-isoquinoline-acetamide, 3,4- dihydro- 6,7- dimethoxy- α - phenyl- N,N- bis [2- (2,3,4- trimethoxy-phenyl) ethyl]-, monomethanesulfonate (pinokalant, salt form of the active entity LOE 908 BS, CAS 143482-63-7), a nonselectiv
Publikováno v:
Basic Toxicology. 96:316-324
Activation of cation channels conducting Ca2+, Na+ and K+ is involved in the pathogenesis of infarction in experimental focal cerebral ischaemia. Pinokalant (LOE 908 MS) is a novel broad-spectrum inhibitor of several subtypes of such channels and has
Autor:
Klaus Mendla, Andreas Raschig, Helmut Ensinger, Thomas Weiser, Wolfram Gaida, Takeshi Osugi, Angelo Ceci, Marion Wienrich
Publikováno v:
Drug Development Research. 56:321-334
Since the discovery of muscarinic receptor subtypes, extensive research has been going on attempting to provide treatments for diseases related to malfunctions of cholinergic receptors. In Alzheimer's disease, the prevailing symptomatology is a progr
Autor:
Andreas Raschig, Wolfram Gaida, D. Meier, Rudolf Hammer, Helmut Ensinger, Marion Wienrich, A. Walland
Publikováno v:
Life Sciences. 68:2593-2600
In functional pharmacological assays, talsaclidine has been described as a functionally preferential M1 agonist with full intrinsic activity, and less pronounced effects at M2- and M3 receptors. In accordance with this, cholinomimetic central activat
Autor:
Kathryn E. Saatman, Jessica A. Cheney, Ramesh Raghupathi, Adrienne L. Brown, Justin D. Weisser, Helmut Ensinger, Florence M. Bareyre, Andrew B. Russ, Andreas Leusch
Publikováno v:
Journal of Neurotrauma. 17:83-91
Experimental traumatic brain injury (TBI) initiates massive disturbances in Ca2+ concentrations in the brain that may contribute to neuronal damage. Intracellular Ca2+ may be elevated via influx through voltage-operated cation channels, ligand-gated
Publikováno v:
Journal of Medicinal Chemistry. 40:2922-2930
We have synthesized a series of stereoisomeric 6,7-benzomorphan derivatives with modified N-substituents and determined their ability to antagonize the N-methyl-D-aspartate (NMDA) receptor-channel complex in vitro and in vivo. The ability of the comp
Autor:
Joachim Mierau, Wolf‐Dieter Bechtel, Klaus Mendla, Wolfgang Tröger, Helmut Ensinger, Franz Birke, Georg Speck
Publikováno v:
Drug Development Research. 40:144-157
The functional selectivity of WAL 2014 FU with regard to stimulation of the neuronal muscarinic M1 receptor subtype in vitro and in vivo is shown in different receptor preparations, isolated organ models, whole animal testing, and finally humans. Fro
Autor:
Mary E. Lajiness, Christopher L. Chio, Helmut Ensinger, Joachim Mierau, Rita M. Huff, Franz J. Schneider
Publikováno v:
European Journal of Pharmacology: Molecular Pharmacology. 290:29-36
Pramipexole (SND 919; 2-amino-4,5,6,7-tetrahydro-6-propylamino-benzthiazole-dihydrochlor ide) is a potent dopamine autoreceptor agonist. We have carried out an analysis of the binding affinities of dopamine D2L, D2S, D3, and D4 receptors for pramipex
Autor:
Gilbert Vassart, Helmut Ensinger, Jacqueline Van Sande, Frédérick Libert, Anne Lefort, Klaus Mendla, Jacques Emile Dumont, Armin Czernilofsky
Publikováno v:
Biochemical and Biophysical Research Communications. 187:919-926
A human brain hippocampus cDNA library was screened by hybridization with a dog A1 adenosine receptor cDNA probe. Sequencing of the resulting clones identified a 978 residue open reading frame encoding a 326 amino acid polypeptide showing 95.7% simil
Autor:
Klaus Mendla, Helmut Ensinger, Angelo Sagrada, Henri Doods, F.J. Kuhn, A. Immel-Sehr, Ernst Mutschler, Günter Lambrecht, G. Walther, Rudolf Hammer, R.E. Müller
Publikováno v:
Life sciences. 52(5-6)
The ability of WAL 2014 to elicit muscarinic responses was investigated in various in vitro and in vivo models. In CHO cells transfected with human m1- or m3-receptor genes, WAL 2014 was clearly more effective in stimulating the M1-mediated PI respon