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10 results on '"Gönne, S."'

1. Abstracts of the sixth international conference on experimental ulcer

Author

Aho, P., Lindén, I. -B., Nissinen, E., Pohto, P., Arvidsson, Stefan, Carter, Katharine, Silen, William, Avunduk, C., Polakouski, N. J., Quimby, G. F., Eastwood, G. L., Batzri, Shmuel, Bank, S., Greenberg, R. E., Kranz, V., Ilardl, C., Chemer, J. A., Singh, G., Naik, L., Chiverton, S. G., Hunt, R. H., Dammann, H. G., Kangah, R., Dreyer, M., Müller, P., Simon, B., Ezer, E., Fändriks, L., Jönson, C., Lisander, B., Frydman, G., O'Brien, P., Phelan, D., Flemström, G., Holmes, R., Malcontenti, C., Gompertz, R. H., Man, W. K., Li, S. K., Baron, J. H., Spencer, J., Michalowski, A. S., Gyires, Klara, Kovacs, Aniko, Gutknecht, John, Inauen, W., Rohner, C., Koelz, H. R., Herdmann, J., Schürer-Maly, C. C., Halter, F., Harmon, John, Hakki, Faris, Malthaner, Richard, Saini, Nirmal, Tay, Howard, Japundžić, L., Levi, E., Rakić, Lj., Holzer, P., Lippe, I. Tb., Pabst, H. A., Lorbach, M., Xing, L., Washington, J., Kauffman, G., Kawamura, Takeshi, Koizumi, Fumiaki, Ishimori, Akira, Kivilaakso, E., Kiviluoto, T., Mustonen, H., Konturek, S. J., Brzozowski, T., Dembinski, A., Uarzecha, Z., Konturek, J. W., Bielanski, W., Bogdał, J., Oleksy, J., Krämling, H. -J, Wiesinger, H., Merkle, T., Merkle, R., Enders, G., Drozdowicz, D., Garlicki, J., Kromer, W., Gönne, S., Lam SK, Chen BW, Hul WM, Ng MMT, Cho CH, Luk CT, Ligumsky, M., Sestieri, M., Karmeli, F., Rachmilewitz, D., Evangelista, S., Rovero, P., Mózsik, Gy., Fiegler, M., Garamszegi, M., Jáyor, T., Nagy, L., Sütő, G., Vincze, Á., Odes, HS, Hogan, DL, Ballesteros, MA, Wolosin, JD, Koss, MA, Isenberg, JI, Jávor, T., Vinoze, A., Steinbach, JH, Okabe, S., Kuwahara, Y., Nishida, T., Wang, J. Y., Nagai, H., Takeuchi, K., Palitzsch, K. D., Szabo, S., Pettersson, A., Peitsch, W., Lange, W., Parekh, D., Segal, I., Lawson, H. H., van der Walt, L. A., Sewing, K. -Fr., Beinborn, M., Seidler, U., Jansons, R., Silen, W., Spill, W. F., Pihan, G., Starlinger, H., Schiessel, R., Wenzl, E., Feil, W., Taché, Yvette, Keshavarzian, A., Wibowo, A., Fields, J. Z., Koji-Takeuchi, Nishiwaki, Hideyuki, Okabe, Susumu, Okada, Megumu, Niida, Hiromiti, Takeuchi, Koji, Vantrappen, G., Tarnawski, A., Hollander, D., Krause, W. J., Gergely, H., Yahav, J., Fradkin, A., Diver-Haber, A., Jonas, A., Allen, A., Leonard, A. J., and Pearson, J. P.

Published
1988
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5. BY 1023/SK&F 96022 INN pantoprazole, a novel gastric proton pump inhibitor, potently inhibits acid secretion but lacks relevant cytochrome P450 interactions.

Author

Kromer, W, Postius, S, Riedel, R, Simon, W A, Hanauer, G, Brand, U, Gönne, S, and Parsons, M E

Abstract

The novel H+/K(+)-adenosine triphosphatase inhibitor (gastric proton pump inhibitor), BY 1023/SK&F 96022, was found to be more potent than omeprazole in some rat models and slightly less potent in a dog model. Overall, both compounds are of a similar potency and efficacy. BY 1023/SK&F 96022 exhibited a somewhat longer duration of the antisecretory action than omeprazole in the Ghosh-Schild rat. In the modified Shay rat, on the basis of equieffective doses in terms of the initial effect, both compounds had a comparable duration of action. However, the p.o./i.v. dose ratio upon acute administration was larger for omeprazole, possibly reflecting its lower stability in the acidic environment of the secreting stomach, compared to BY 1023/SK&F 96022. As in vivo, both compounds were equipotent to inhibit acid production in rabbit isolated fundic glands. However, omeprazole interacted with the 7-ethoxycoumarin dealkylase in vitro with high affinity (Ki = 38.5 mumol/l), in contrast to BY 1023/SK&F 96022 (Ki = 135 mumol/l). Compared to omeprazole, BY 1023/SK&F 96022 also showed less interaction with the cytochrome P450 enzyme hydroxylating ionazolac. Moreover, this difference between the two compounds was also found in the rat in vivo with respect to their interaction with diazepam. Thus, both compounds displayed a comparable antisecretory potency in vivo and in vitro but showed a different interference with cytochrome P450 in favor of less interaction by BY 1023/SK&F 96022.

Published
1990

7. Sila-Procyclidin: Eine neue Synthese sowie Untersuchungen zur peripheren und zentralen anticholinergen Wirkung

Author

Tacke, Reinhold, Pikies, J., Linoh, H., Rohr-Aehle, R., and Gönne, S.

Subjects
ddc:540, Anorganische Chemie
Abstract

Sila-Procyclidin (1 b) sowie dessen Derivate 2b (Sila-Tribexyphenidyl), 3b und 4b (Sila-Cycrimin) wurden - ausgehend von Cl\(_3\)SiCH\(_2\)Cl - durch eine neue, sechsstufige Synthese mit einer Gesamtausbeute von 16 (lb), t9 (2b), 8 (3b) bzw. 7% (4b) dar· gestellt. - Vergleichende in-vivo-Untcrsuchungen (Maus, per-osApplikation) hinsichtlich der peripheren und zentralen auticholincrgen Wirkung haben gezeigt, daß die Silicium-Verbindung 1 b dem Kohlenstoff-Analogon Ia (Procyclidin) überlegen ist., Starting with Cl\(_3\)SiCH\(_2\)Cl. sila-procycUdine (I b) as well as its derivatives 2b (sila-trihexyphenidyl), 3b, and 4b (sila-cycrimine) were prepared by a new six-step synthesis witb a total yield of 16 (lb), 19 (2b), 8 (31) aud 7% (4b), respectively. - Comparative in vivo investigations (mice per os administration) with respect to the peripheral and centrat anticholinergic activity bavc shown that the silicon compound 1 b is advantageous over the c:arbon aualogue t a (procyclidine).

Published
1987

9. [Studies on the effect of urapidil on the central nervous system and various organ functions in animal experiments (author's transl)].

Author

Schoetensack W, Eltze M, Gönne S, Kley KP, Menge HG, and Müller H

Subjects
Animals, Avoidance Learning drug effects, Behavior, Animal drug effects, Blood Pressure drug effects, Cats, Decerebrate State, Electroencephalography, Female, Guinea Pigs, Hypnotics and Sedatives, In Vitro Techniques, Male, Mice, Motor Activity drug effects, Muscle Contraction drug effects, Muscle, Smooth drug effects, Rats, Reflex drug effects, Uracil pharmacology, Antihypertensive Agents pharmacology, Central Nervous System drug effects, Uracil analogs & derivatives
Abstract

Compared to the changes in spontaneous behaviour of mice and rats, 6-(3-[4-(o-methoxyphenyl)-1-piperazinyl]-propyl-amino)-1,3-dimethyluracil (urapidil, Ebrantil) in doses from 10 mg/kg p.o. has a central sedative action, for which it is typical that it can be interrupted by external stimuli after doses of up to approx. 100 mg/kg. By this action urapidil differs from other central-acting drugs, e.g. chlor-promazine, diazepam and clonidine. It can be assumed that urapidil has no central dopamine blocking qualities because it does neither influence the conditioned avoidance response nor the amphetamine-induced gnawing of the rat. Urapidil is also different from diazepam bacause it does not hinder spinal polysynaptic motor reflexes of the decerebrated cat. Up to 80 mg/kg p.o. of urapidil, there was no hypotensive effect in the rat to be seen and, therefore, it can be concluded that changes in spontaneous and reactive behaviour are not due to acute changes in cardiovascular functions. The antihistamine effect of urapidil in the isolated ileum of the guinea pig is approx. 15 times weaker than that of chlorpromazine, furthermore urapidil has no anticholinergic quality.

Published
1977

10. Pharmacological evidence for selective inhibition of gastric acid secretion by telenzepine, a new antimuscarinic drug.

Author

Eltze M, Gönne S, Riedel R, Schlotke B, Schudt C, and Simon WA

Subjects
Aminopyrine metabolism, Animals, Dogs, Female, Gastric Mucosa drug effects, Guinea Pigs, In Vitro Techniques, Male, Mice, Muscle Contraction drug effects, Muscle, Smooth drug effects, Myocardial Contraction drug effects, Rabbits, Rats, Rats, Inbred Strains, Receptors, Muscarinic drug effects, Stomach drug effects, Urinary Bladder drug effects, Benzodiazepinones pharmacology, Gastric Acid metabolism, Parasympatholytics pharmacology, Pirenzepine analogs & derivatives
Abstract

The new antisecretory drug, telenzepine (4,9-dihydro-3-methyl-4-[(4-methyl-1-piperazinyl)acetyl]-10H-thieno-[3,4 - b][1,5]benzodiazepin-10-one), was investigated for its inhibition of functionally intact muscarinic receptors involved in gastric acid secretion in rabbit fundic glands, perfused mouse stomach in vitro, perfused rat stomach in situ, gastric fistula in rats and dogs with a Heidenhain pouch. The effects on these receptors were contrasted with effects on receptors located on smooth muscle and heart, i.e. isolated rat urinary bladder, stomach and atrium. The results were compared to those values obtained with nonselective antimuscarinic drugs (N-methylscopolamine, atropine) and the selective M-1 antagonist pirenzepine. Telenzepine was found to be 4-10 times more potent than pirenzepine with respect to depressing both gastric acid secretion and smooth muscle or myocardial responses. Based on -log EC50 and pA2 values, both drugs exhibited a similar selectivity profile differing from the pattern of effects observed with atropine or a second reference compound, zolenzepine. As compared with atropine, telenzepine exhibited a 5 fold higher relative affinity to muscarinic receptors involved in gastric acid secretion. It was concluded that telenzepine is selective to discriminate between muscarinic receptors mediating gastric acid secretion and affecting muscle contractility and that this finding supports the concept of muscarinic receptor heterogeneity.

Published
1985
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