TY  - THES
A1  - Handmann, Vera Iris
T1  - Studien zur C/Si-Bioisosterie
T1  - Studies on C/Si Bioisosterism
N2  - Im Rahmen der vorliegenden Arbeit wurden Beiträge zur C/Si-Bioisosterie und zur asymmetrischen Synthese neuer siliciumhaltiger alpha-Aminosäuren geleistet. Im Vordergrund der Untersuchungen stand die Entwicklung neuer präparativer Methoden zur Darstellung siliciumhaltiger Wirkstoffe und die Untersuchung ihrer pharmakologischen Wirksamkeit sowie die Synthese racemischer und enantiomerenreiner siliciumhaltiger alpha-Aminosäuren des beta-(Trimethylsilyl)alanin-Typs.
N2  - This work describes contributions to the field of C/Si bioisosterism and to the asymmetric synthesis of novel silicon-containing alpha-amino acids. The aim of these investigations was the development of new preparative methods for the synthesis of silicon-containing drugs and their pharmacological evaluation as well as the synthesis of racemic and enantiomerically pure silicon-containing alpha-amino acids of the beta-(trimethylsilyl)alanine type.
KW  - Kohlenstoff
KW  - Silicium
KW  - Bioisosterie
KW  - Muscarin
KW  - Antagonist
KW  - Aminosäurederivate
KW  - Aminosäuren
KW  - Antipsychotika
KW  - Bioanorganik
KW  - Kristallstrukturanalyse
KW  - Muscarin Antagonisten
KW  - pharmakologisches Profil
KW  - Silicium
KW  - Synthese
KW  - amino acids
KW  - antipsychotics
KW  - bioinorganic chemistry
KW  - C/Si bioisosterism
KW  - crystal structure analysis
KW  - muscarinic antagonists
Y1  - 2002
U6  - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-4719
ER  - 
TY  - JOUR
A1  - Jaiswal, Neelam
A1  - Lambrecht, Günter
A1  - Mutschler, Ernst
A1  - Tacke, Reinhold
A1  - Malik, Kafait U.
T1  - Pharmacological characterization of the vascular muscarinic receptors mediating relaxation and contraction in rabbit aorta
JF  - Journal of Pharmacology and Experimental Therapeutics
N2  - Studies were performed in the rabbit aortic rings, precontracted with norepinephrine, to determine the subtype(s) of muscarinic receptors involved in endothelium-dependent relaxation and contraction in the absence of endothelium elicited by cholinergic stimuli. Acetylcholine (ACh) and arecaidine propargyl ester (APE), a M2 and M3 agonist, produced a dose-dependent relaxation and contraction in endothelium-intact and endothelium-denuded rabbit aortic rings, respectively. Both of these responses were blocked by the muscarinic receptor antagonist atropine. M1 selective agonist McN-A-343 [4-[N-(3-chlorophenyl)carbamoyloxy]-2-butinyltrimethylammonium+ ++ chloride] did not produce any effect on the tone of precontracted aortic rings. ACh- and APE-induced relaxation in aortic rings with intact endothelium was selectively blocked by M3 receptor antagonists hexahydrosila-difenidol and p-fluoro-hexahydro-sila-difenidol (pA2 of 7.84 and 7.18) but not by M1 antagonist pirenzepine or M2 receptor antagonists AF-DX 116 [11-(2-[(diethylamino)methyl]- 1-piperidinyl]acetyl)-5, 11-dihydro-6H-pyrido-[2,3-b][1,4]-benzo-diazepin-6-one] and methoctramine. ACh- and APE-induced contraction was inhibited by M2 receptor antagonists AF-DX 116 and methoctramine (pA2 of 7.11 and 6.71) but not by pirenzepine, hexahydro-sila-difenidol or p-fluoro-hexahydro-sila-difenidol. ACh- and APE-induced relaxation or contraction were not altered by nicotinic receptor antagonist hexamethonium or cyclooxygenase inhibitor indomethacin. These data suggest that relaxation elicited by cholinergic stimulin in endothelium-intact aortic rings is mediated via release of endothelium-derived relaxing factor consequent to activation of M3 receptors located on endothelial cells, whereas the contraction in aortic rings denuded of their endothelium is mediated via stimulation of M2 receptors located on smooth muscle cells.
KW  - (4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chloride/pharmacology
KW  - acetylcholine
KW  - animals
KW  - antihypertensive agents / pharmacology
KW  - aorta, abdominal / drug effects
KW  - aorta, abdominal / physiology
KW  - aorta, abdominal / ultrastructure
KW  - arecoline/analogs & derivatives
KW  - arecoline
KW  - atropine
KW  - diamines
KW  - endothelium, vascular / drug effects
KW  - endothelium, vascular / physiology
KW  - hexamethonium
KW  - hexamethonium compounds
KW  - indomethacin
KW  - male
KW  - muscarinic antagonists
KW  - muscle contraction
KW  - muscle relaxation
KW  - norepinephrine
KW  - parasympatholytics
KW  - piperidines
KW  - pirenzepine
KW  - rabbits
Y1  - 1991
U6  - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-128358
VL  - 258
IS  - 3
ER  - 
TY  - JOUR
A1  - Tacke, Reinhold
A1  - Kropfgans, Martin
A1  - Tafel, Andrea
A1  - Wiesenberger, Frank
A1  - Sheldrick, William S.
A1  - Mutschler, Ernst
A1  - Egerer, Hansjörg
A1  - Rettenmayr, Nikola
A1  - Gross, Jan
A1  - Waelbroeck, Magali
A1  - Lambrecht, Günter
T1  - (Hydroxymethyl)diphenyl(piperidinoalkyl)silane des Typs (HOCH2)(C6H5)2Si(CH2)nNC5H10 (n = 2,3) und deren Methoiodide: Synthese, Struktur und antimuscarinische Eigenschaften
N2  - No abstract available.
KW  - (Hydroxymethyl)diphenyl(piperidinoalkyl)silanes
KW  - Sila-pridinol
KW  - Sila-difenidol
KW  - muscarinic antagonists
KW  - muscarinic receptors
Y1  - 1994
U6  - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-86904
ER  -