Search Results - "Ensinger, H A"

BIIR 561 CL: a novel combined antagonist of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors and voltage-dependent sodium channels with anticonvulsive and neuroprotective properties by Weiser, T, Brenner, M, Palluk, R, Bechtel, W D, Ceci, A, Brambilla, A, Ensinger, H A, Sagrada, A, Wienrich, M

“…Antagonists of glutamate receptors of the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) subtype, as well as of voltage-gated sodium channels,…”
Get more information

Therapeutic potential of CNS-active M2 antagonists: novel structures and pharmacology by Doods, H N, Quirion, R, Mihm, G, Engel, W, Rudolf, K, Entzeroth, M, Schiavi, G B, Ladinsky, H, Bechtel, W D, Ensinger, H A

“…Clinical trials with muscarinic agonists or acetylcholine esterase inhibitors for the treatment of Alzheimer's dementia have shown disappointing or equivocal…”
Get more information

Cloning and functional characterization of a human A1 adenosine receptor by Libert, F, Van Sande, J, Lefort, A, Czernilofsky, A, Dumont, J E, Vassart, G, Ensinger, H A, Mendla, K D

“…A human brain hippocampus cDNA library was screened by hybridization with a dog A1 adenosine receptor cDNA probe. Sequencing of the resulting clones identified…”
Get more information

The novel compound LOE 908 attenuates acute neuromotor dysfunction but not cognitive impairment or cortical tissue loss following traumatic brain injury in rats by Cheney, J A, Brown, A L, Bareyre, F M, Russ, A B, Weisser, J D, Ensinger, H A, Leusch, A, Raghupathi, R, Saatman, K E

“…Experimental traumatic brain injury (TBI) initiates massive disturbances in Ca2+ concentrations in the brain that may contribute to neuronal damage…”
Get more information

WAL 2014--a muscarinic agonist with preferential neuron-stimulating properties by Ensinger, H A, Doods, H N, Immel-Sehr, A R, Kuhn, F J, Lambrecht, G, Mendla, K D, Müller, R E, Mutschler, E, Sagrada, A, Walther, G

“…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-…”
Get more information

Synthesis and Structure−Activity Relationships of 6,7-Benzomorphan Derivatives as Antagonists of the NMDA Receptor−Channel Complex by Grauert, Matthias, Bechtel, Wolf Dietrich, Ensinger, Helmut A, Merz, Herbert, Carter, Adrian J

“…We have synthesized a series of stereoisomeric 6,7-benzomorphan derivatives with modified N-substituents and determined their ability to antagonize the…”
Get full text

Inhibition by the PAF antagonist WEB 2086 of PAF induced inositol‐1,4,5‐trisphosphate production in human platelets by Birke, F. W., Ensinger, H. A.

“…Platelet‐activating factor (PAF) activates human platelets by binding to a putative PAF receptor which evokes the rapid formation of…”
Get full text

Radioreceptor assay for determination of the antimuscarinic drug ipratropium bromide in man by ENSINGER, H. A, WAHL, D, BRANTL, V

“…A radioreceptor assay for the determination of ipratropium bromide in human plasma has been developed, using [3H] N-methyl-scopolamine as a radioligand to…”
Get full text

Pharmacodynamic profile of the M 1 agonist talsaclidine in animals and man by Wienrich, M., Meier, D., Ensinger, H.A., Gaida, W., Raschig, A., Walland, A., Hammer, R.

“…In functional pharmacological assays, talsaclidine has been described as a functionally preferential M 1 agonist with full intrinsic activity, and less…”
Get full text

In vivo role of the adenosine A3 receptor: N6-2-(4-aminophenyl)ethyladenosine induces bronchospasm in BDE rats by a neurally mediated mechanism involving cells resembling mast cells by Meade, C J, Mierau, J, Leon, I, Ensinger, H A

“…Activation of the adenosine A3 receptor subtype by the agonist N6-2-(4-aminophenyl)ethyladenosine is shown here to induce bronchospasm (increased pulmonary…”
Get more information

Pharmacokinetics of pinokalant, a new nonselective cation channel blocker in the rat by LEUSCH, Andreas, EICHHORN, Bettina, BUSCH, Ulrich, ENSINGER, Helmut A

“…The pharmacokinetics of 1-isoquinolineacetamide, 3,4-dihydro-6,7-dimethoxy-alpha-phenyl-N,N-bis [2-(2,3,4-trimethoxyphenyl)ethyl]-, monomethanesulfonate…”
Get full text

Plasma levels of opioid analgesics determined by radioreceptor assay by Ensinger, H A, Doevendans, J E

“…Plasma levels of opioid drugs, Mr 1268 MS (3-(2-methyl-3-furylmethyl)-1,2,3,4,5,6-hexahydro-6 alpha,11 alpha-dimetyl-2,6-methano-3-benzazocin-8-ol methane…”
Get more information

Differentiation of mu- and kappa-receptors by means of correlation of analgesic potency in vivo and receptor binding affinity in vitro of various opioid agonists by Ensinger, H A, Stockhaus, K, Merz, H

“…For various opioid agonists (n = 35) an unsatisfactory correlation between analgesic activity in vivo (mouse) and receptor binding affinity (rat brain) in…”
Get more information

Biochemical studies with the new thienotriazolo-diazepine brotizolam by Bechtel, W D, Ensinger, H A, Mierau, J

“…Brotizolam (2-bromo-4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f]-1,2,4-triazolo [4,3-a]-1,4-diazepine, We 941, Lendormin) is a newly developed…”
Get more information

Differentiating aspects of opioid receptor binding by [3H](-) (1R,5R,9R,2''S)-5,9-dimethyl-2-tetrahydrofurfuryl-2'-hydroxy-6,7- benzomorphan hydrochloride ([3H]Mr 2034), a drug preferentially acting on kappa-receptors by Ensinger, H A

“…Receptor binding experiments with masking of mu- and delta-receptors in the presence of an excess of unlabelled dihydromorphine and [D-Ala2, D-Leu5]enkephalin…”
Get more information

Mr 2033 CL--a novel non-morphine-like opioid analgesic by Stockhaus, K, Ensinger, H A, Gaida, W, Jennewein, H M, Merz, H

“…Mr 2033 CL is a very potent non-morphine-like opioid analgesic as shown in different test models and animal species. On a weight for weight basis, it is about…”
Get more information

The role of Zn(II) in calf intestinal alkaline phosphatase studied by the influence of chelating agents and chemical modification of histidine residues by Ensinger, H A, Pauly, H E, Pfleiderer, G, Stiefel, T

“…Alkaline phosphatase from calf intestine (orthophosphoric-monoester phosphohydrolase (alkaline optimum), EC 3.1.3.1) is reversibly inhibited at pH 8.0 by…”
Get more information

Pharmacodynamic profile of the M1 agonist talsaclidine in animals and man by Wienrich, M, Meier, D, Ensinger, H A, Gaida, W, Raschig, A, Walland, A, Hammer, R

“…In functional pharmacological assays, talsaclidine has been described as a functionally preferential M1 agonist with full intrinsic activity, and less…”
Get full text

The Broad‐Spectrum Cation Channel Blocker Pinokalant (LOE 908 MS) Reduces Brain Infarct Volume in Rats: A Temperature‐Controlled Histological Study by Christensen, Thomas, Wienrich, Marion, Ensinger, Helmut A., Diemer, Nils Henrik

“…: Activation of cation channels conducting Ca2+, Na+ and K+ is involved in the pathogenesis of infarction in experimental focal cerebral ischaemia. Pinokalant…”
Get full text

Pramipexole binding and activation of cloned and expressed dopamine D2, D3 and D4 receptors by Mierau, J, Schneider, F J, Ensinger, H A, Chio, C L, Lajiness, M E, Huff, R M

“…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…”
Get full text