@article{TackeStreckerSheldricketal.1979, author = {Tacke, R. and Strecker, M. and Sheldrick, W. S. and Heeg, E. and Berndt, B. and Knapstein, K. M.}, title = {Sila-Pharmaka, 14. Mitt. Darstellung und Eigenschaften sowie Kristall-und Molek{\"u}lstruktur von Sila-Difenidol}, series = {Zeitschrift f{\"u}r Naturforschung B}, volume = {34}, journal = {Zeitschrift f{\"u}r Naturforschung B}, number = {9}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-128391}, pages = {1279-1285}, year = {1979}, abstract = {Sila-difenidol (6b), a sila-analogue of the drug difenidol (6a), was synthesized according to Scheme 1. 6b and its new precursors 3 and 5 were characterized by their physical and chemical properties, and their structures confirmed by elementary analyses, 1H NMR and mass spectroscopy. 6 b crystallizes orthorhombic \(P2_12_12_1\) with a = 11.523(1), b = 14.366(4), c = 11.450(1) {\AA}, Z = 4, \(D_{ber} = 1.14 gcm^{-3}\). The structure was refined to R = 0.050 for 1897 reflexions. A strong nearly linear intramolecular O-H···N hydrogen bond of 2.685 {\AA} is observed. The anticholinergic, histaminolytic and musculotropic spasmolytic activities of 6 a and 6 b are reported.}, language = {de} } @article{TackeStreckerSheldricketal.1980, author = {Tacke, Reinhold and Strecker, M. and Sheldrick, W. S. and Ernst, L. and Heeg, E. and Berndt, B. and Knapstein, C.-M. and Niedner, R.}, title = {Sila-Pridinol und Pridinol: Darstellung und Eigenschaften sowie Strukturen im kristallinen und gel{\"o}sten Zustand}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-63654}, year = {1980}, abstract = {Sila-Pridinol (2 b), ein Sila-Analogon des Anticholinergicums Pridinol (2a), wurde auf zwei verschiedenen Wegen dargestellt. Die Kristall- und Molek{\"u}lstrukturen von 2 a und 2 b wurden r{\"o}ntgenstrukturanalytisch bestimmt. 2a bildet im festen Zustand intramolekulare Wasserstoffbr{\"u}ckenbindungen aus, w{\"a}hrend sich in kristallinem 2 b zentrosymmetrische, durch intermolekulare H-Br{\"u}ckenbindungen verkn{\"u}pfte cyclische Dimere finden. IR- und \8^1\)H-NMR-spektroskopische sowie kryoskopische Untersuchungen ergaben Informationen {\"u}ber die Strukturen von 2a und 2 b in verschiedenen L{\"o}sungsmitteln. - Die pharmakologischen und toxikologischen Eigen" schaften von 2a und 2b wurden unter dem Gesichtspunkt bekannter Struktur-Wirkungs-Beziehungen vergleichend untersucht. 2 b erwies sich als ein etwa f{\"u}nfmal so starkes Anticholincrgicum wie 2a.}, subject = {Anorganische Chemie}, language = {de} } @article{TackeZimonyiHegeduesStreckeretal.1980, author = {Tacke, Reinhold and Zimonyi-Heged{\"u}s, E. and Strecker, M. and Heeg, E. and Berndt, B. and Langner, R.}, title = {Sila-Analogon des Tiemoniumiodids}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-63669}, year = {1980}, abstract = {Sila-Tiemoniumiodid (16b), ein Sila-Analogon des Anticholinergicums Tiemoniumiodid (16a), und das Sila-Analogon 14b der entsprechenden Tiemonium-Base 14a wurden erstmalig synthetisiert.14b und 16b sowie die Vorstufen 10-13 und 15 wurden in ihren physikalischen und chemischen Eigenschaften charakterisiert und in ihrer Struktur durch Elementaranalysen sowie \(^1\)H-NMR- und Massenspektren sichergestellt. Die spasmolytischen Eigenschaften der Paare 14a/14b und 16a/16b wurden am isolierten Meerschweinchendarm vergleichend untersucht.}, subject = {Anorganische Chemie}, language = {de} } @article{TackeLangeAttarBashi1982, author = {Tacke, Reinhold and Lange, H. and Attar-Bashi, M. T.}, title = {Baseninduzierte 1,2-Hydridverschiebungen vom Silicium zum Kohlenstoff: "Anomale" Substitutionsreaktionen an (Halogen-methyl)diorganylsilanen}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-63734}, year = {1982}, abstract = {(C\(_6\)H\(_5\))\(_2\)Si(H)CH\(_2\)X (1 a: X = Cl; 1 b: X = I) und C\(_6\)H\(_5\)(CH\(_3\))Si(H)CH\(_2\)CI (10) reagieren mit LiOCH\(_2\)CH\(_2\)N(CH\(_3\))\(_2\) (2b) zu den Alkoxysilanen (C\(_6\)H\(_5\))\(_2\)Si(CH\(_3\))OCH\(_2\)CH\(_2\)N(CH\(_3\))\(_2\) (5) bzw. C\(_6\)H\(_5\)(CH\(_3\))\(_2\)SiOCH\(_2\)CH\(_2\)N(CH\(_3\))\(_2\) (12). Die Bildung dieser unerwarteten Reaktionsprodukte wird durch einen nucleophilen Angriff des Alkoxids am Si-Atom gedeutet. dem sich eine intramolekulare 1 ,2-Hydridverschiebung vom Si zum C und Eliminierung von Cl e anschließt. Mit weichen Basen, wie z. B. I (-) und (-)SCH\(_2\)CH\(_2\)N(CH\(_3\))\(_2\), wurden dagegen "normale" Substitutionsreaktionen am C-Atom der SiCH\(_2\)Cl-Gruppe beobachtet}, subject = {Anorganische Chemie}, language = {de} } @article{TackeStreckerLambrechtetal.1983, author = {Tacke, Reinhold and Strecker, M. and Lambrecht, G. and Moser, U. and Mutschler, E.}, title = {(2-Aminoethyl)-cycloalkylphenylsilanole: Bioisosterer C/Si-Austausch bei Parasympatholytika vom Typ des Trihexyphenidyls, Cycrimins und Procyclidins}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-63741}, year = {1983}, abstract = {Die Synthese der (2-Aminoethyl)cycloalkylphenylsilanole Sb (Sila-Trihexyphenidyl), 6b (SilaCycrimin), 7 b (Sila-Procyclidin) und Sb wird beschrieben. Sb- Sb wurden - ausgehend von Cl\(_2\)(C\(_6\)H\(_5\))SiCH = CH\(_2\) (9) - durch eine f{\"u}nfstufige Reaktionsfolge mit einer Gesamtausbeute von 32- 40\% erhalten. Am isolierten Ileum des Meerschweinchens wurden die C/Si-Paare Sa, b- 8a, b vergleichend auf ihre antimuskarinische Aktivit{\"a}t gepr{\"u}ft. Die durch die Sila-Substilution von Sa-8a erreichte Zunahme der Affinit{\"a}t zum Muskarinrezeptor ist deutlich weniger ausgepr{\"a}gt als bei den strukturverwandten C/Si-Paaren I a, b- 4a, b.}, subject = {Anorganische Chemie}, language = {de} } @article{TackeStreckerLambrechtetal.1984, author = {Tacke, Reinhold and Strecker, M. and Lambrecht, G. and Moser, U. and Mutschler, E.}, title = {Bioisosterer C/Si-Austausch bei Parasympatholytika vom Typ des Pridinols}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-63766}, year = {1984}, abstract = {Die Synthese der (2·Aminoethyl)diphenylsilanole 3b und 4b wird beschrieben. Die parasympatholytischen Eigenschaften der CISi-Paare la/lb-4a/4b wurden am isolierten Ileum des Meerschweinchens untersucht. In allen F{\"a}llen f{\"u}hrt der C/Si-Austausch zu einer Zunahme der Affinit{\"a}t zum Muskarin-Rezeptor.}, subject = {Anorganische Chemie}, language = {de} } @article{EltzeUllrichMutschleretal.1993, author = {Eltze, M. and Ullrich, B. and Mutschler, E. and Moser, U. and Bungardt, E. and Friebe, T. and Gubitz, C. and Tacke, Reinhold and Lambrecht, G.}, title = {Characterization of muscarinic receptors mediating vasodilation in rat perfused kidney}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-64283}, year = {1993}, abstract = {The muscarinic receptor mediating vasodilation of resistance vessels in the rat isolated, constant-pressure perfused kidney (preconstriction by w- 7 M cirazoline) was characterized by subtype-preferring agonists and se]ective antagonists. The agonists produced vasodi1ation with the fol1owing rank order of potency: arecaidine propargy] ester (APE) > 5-methylfurtrethonium = methacholine = oxotremorine > (S)-aceclidine > arecaidine 2-butyne-1,4-diyl bisester > 4-Cl-McN-A-343 = (R)-nipecotic acid ethyl ester = N-ethyl-guvacine propargyl ester- (R)-aceclidine = (S)-nipecotic acid ethyl ester > McN-A-343. Agonist-induced vasodilation disappeared after destruction of the endothelium with detergent. Highly significant correlations of agonist potencies for vasodilation were found between rat kidney and guinea-pig ileum submucosal arterioles as weH as agonist potencies at smooth muscle muscarinic M\(_3\) receptors of the guinea-pig ileum. The rank order of antagonist potencies (4-diphenylacetoxy-Nmethylpiperidine methiodide (4-DAMP) > (R)-hexahydro-difenidol - hexahydro-sila-difenidol > pirenzepine - p-fluorohexahydro- sila-difenidol- himbacine- AF-DX 384- AQ-RA 741 > (S)-hexahydro-difenidol) to attenuate vasodilation to APE in rat kidney, correlated significantly with affinities at M\(_3\) receptors in submucosal arterioles and in smooth muscle of the guinea-pig ileum, but differed from those at M\(_1\) and M\(_2\) receptors in rabbit vas deferens. The agonist and antagonist potencies suggest that vasodilation elicited by muscarinic stimuli in endothelium-intact rat renal vasculature is mediated by functional muscarinic M\(_3\) receptors.}, subject = {Anorganische Chemie}, language = {en} } @article{MuehleisenTacke1994, author = {M{\"u}hleisen, M. and Tacke, Reinhold}, title = {Twofold deprotonated citric acid as a bidentate ligand of pentacoordinate silicon: synthesis and structural characterization of the zwitterionic \(\lambda_5\)Si-spirosilicate bis[citrato(2-)-O\(^3\),O\(^4\)][(dimethylammonio)methyl]silicate hydrate}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-64388}, year = {1994}, abstract = {The zwitterionic \(\lambda_5\) Si-spirosilicate bis[ citrato(2-)-0\(^3\) ,0\(^4\) )[ ( dimethylammonio) methyl]silicate (4) was synthesized by reaction of (MeO)\(_3\)SiCH\(_2\)NMe\(_2\) (3) with citric acid (molar ratio 1 :2) in acetonitrile at room temperature and isolated, after crystallization from water, as the hydrate 4 · H\(_2\)O (yield 81 \%). The crystal structure of 4 · H\(_2\)O was studied by single-crystal X-ray diffraction. The alcoxide oxygen atoms and central carboxylate oxygen atoms of two citrato(2-) ligands and one carbon atom coordinate to the silicon atom of 4 · H\(_2\)O. The coordination polyhedron around the pentacoordinate silicon atom (SiO\(_4\)C framework) can be described as a distorted trigonal bipyramid, the two carboxylate oxygen atoms occupying the axial sites. The \(\lambda_5\) Si~silicon(IV) complex 4 also exists in solution (DMSO, H\(_2\)O).}, subject = {Anorganische Chemie}, language = {de} } @article{MuehleisenTacke1994, author = {M{\"u}hleisen, M. and Tacke, Reinhold}, title = {meso-[1,4-Piperaziniumdiylbis(methylene)]bis{bis[2-methyllactato(2-)-O1,O2]silicate} octahydrate: synthesis and crystal structure analysis of a zwitterionic dispirocyclic \(\lambda^5\)Si,\(\lambda^5\)Si'-disilicate}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-64396}, year = {1994}, abstract = {The zwitterionic dispirocyclic \(\lambda^5\)Si,\(\lambda^5\)Si'-disilicate meso-[1 ,4-piperaziniumdiylbis( methylene)]bis{ bis[ 2-methyllactato(2-)-O\(^1\),O\(^2\)]silicate} octahydrate (6-8H\(_2\)O) was synthesized by reaction of 1,4-bis[(trimethoxysilyl}methyl] piperazine (8) with 2-methyllactic acid (molar ratio 1:4) in water/acetone (yield 82\%). The molecular dinuclear silicon(IV) complex 6 contains two pentacoordinate (formally negatively charged) silicon atoms and two tetracoordinate (formally positively charged) nitrogen atoms. The crystal structure of 6•8H20 was studied by X-ray diffraction.}, subject = {Anorganische Chemie}, language = {en} } @article{TackeMuehleisen1994, author = {Tacke, Reinhold and M{\"u}hleisen, M.}, title = {Bis[benzilato(2-)-O\(^1\),O\(^2\)][2-(dimethylammonio)ethoxy]silicate: synthesis and structural characterization of a zwitterionic \(\lambda^5\)Si-silicate with a SiO\(_5\) framework}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-64400}, year = {1994}, abstract = {No abstract available}, subject = {Anorganische Chemie}, language = {en} } @article{TackePikiesWiesenbergeretal.1994, author = {Tacke, Reinhold and Pikies, J. and Wiesenberger, F. and Ernst, L. and Schomburg, D. and Waelbroeck, M. and Christophe, J. and Lambrecht, G. and Gross, J. and Mutschler, E.}, title = {Sila-biperiden und endo-Sila-biperiden: Synthesen, Kristallstrukturen und antimuscarinische Eigenschaften}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-64303}, year = {1994}, abstract = {Starting from trichloro(vinyl)silane (Cl\(_3\)SiCH=CH\(_2\)), the musearinic antagonists sila-biperiden [rac-(SiRS,C2SR>-ao-2] and endosila- biperiden [rac-(SiRS,C2SR)-endo-2] were prepared by a seven-step synthesis. Both silanols are configurationally stableininert organic solvents but undergo slow epimerization in aqueous solution (pH 7.4, 32°C) by inversion of the configuration at the silicon atom. The relative configurations of sila-biperiden and endo-sila-biperiden were detennined by single-crystal X-ray diffraction. Both compounds form intennolecular 0-H · · · N hydrogen bonds in the crystal leading to the fonnation of centrosymmetric dimers (sila-biperiden) and infinite chains (endo-sila-biperiden), respectively. Sila-biperiden is a silicon analogue (C/Si exchange) of the antiparkinsonian drug biperiden [rac-(CRS/C2SR}-exo-1]. In functional phannacological experiments, as well as in radioligand competition studies, biperiden, sila-biperiden and endo-sila-biperiden behaved as simple competitive antagonists at muscarinic Ml-, M2-, M3- and M4-receptors. The three compounds displayed the highest affinity for Ml-receptors (pA\(_2\) values: 8.72-8.80; pK\(_i\) values: 8.8-9.1), intermediate affinity for M4- and M3-receptors, and lowest affinity for M2-receptors (pA\(_2\) values: 7.57-7.79; pK\(_i\) values: 7.7-7.8). The affinity profile (Ml >. M4 > M3 > M2) of biperiden, sila-biperiden and endo-sila-biperiden is qualitatively similar to that of the M1-selective muscarinic antagonist pirenzepine. The antimuscarinic properlies of the C/Si analogues biperiden and sila-biperiden are almost identical.}, subject = {Anorganische Chemie}, language = {en} } @article{TackeMuehleisenJones1994, author = {Tacke, Reinhold and M{\"u}hleisen, M. and Jones, P. G.}, title = {Das erste zwitterionische, optisch aktive Disilicat mit pentakoordiniertem Silicium}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-64343}, year = {1994}, abstract = {No abstract available}, subject = {Anorganische Chemie}, language = {de} } @article{TackeMuehleisenJones1994, author = {Tacke, Reinhold and M{\"u}hleisen, M. and Jones, P. G.}, title = {The first zwitterionic, optically active disilicate with pentacoordinate silicon}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-64358}, year = {1994}, abstract = {No abstract available}, subject = {Anorganische Chemie}, language = {en} } @article{TackeMuehleisen1994, author = {Tacke, Reinhold and M{\"u}hleisen, M.}, title = {Hexakoordiniertes Silicium in einer molekularen Verbindung mit einer F\(_5\)SiC-Einheit}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-64365}, year = {1994}, abstract = {No abstract available}, subject = {Anorganische Chemie}, language = {de} } @article{TackeMuehleisen1994, author = {Tacke, Reinhold and M{\"u}hleisen, M.}, title = {Hexacoordinate silicon in a compound with an F\(_5\)SiC unit}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-64378}, year = {1994}, abstract = {No abstract available}, subject = {Anorganische Chemie}, language = {en} } @article{TackeLinkZilch1985, author = {Tacke, Reinhold and Link, M. and Zilch, H.}, title = {Eine neue in situ-Darstellung von (Trimethyl-silyl)trifluormethansulfonat durch thermisch induzierte Umlagerung}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-63784}, year = {1985}, abstract = {A new in situ preparation of trimethylsilyl trifluoromethanesulfonate (3) is described: 3 is generated by a thermally induced rearrangement of (dimethylsilyl)methyl trifluoromethanesulfonate (2), which can be prepared by reaction of (CH\(_3\))\(_2\)Si(H)CH\(_2\)OH (1) with (CF\(_3\)SO\(_2\))\(_2\)O. Starting with C\(_6\)H\(_5\)(CH\(_3\))Si(H)CH\(_2\)OH (5), the derivative (methylphenylsilyl)methyl trifluoromethanesulfonate (6) can be obtained by a similar method. Its thermally induced rearrangement Ieads to dimethylphenylsilyl trifluoromethanesulfonate (7). The rearrangements 2---> 3 and 6---> 7 were found to be first-order reactions with half-lifes at 80 oc of 0.75 and 1.7 h, respectively.}, subject = {Anorganische Chemie}, language = {de} } @article{SchomburgLinkLinohetal.1988, author = {Schomburg, D. and Link, M. and Linoh, H. and Tacke, Reinhold}, title = {Molek{\"u}lstruktur der Akarizide Chlortrineophylstannan, Chlortris[(dimethylphenylsilyl)methyl]stannan und Trineophyl(1,2,4-triazol-1-yl)stannan-hemihydrat sowie des 2,5-Dimethyl-2,5-diphenylhexans (Bineophyl)}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-63840}, year = {1988}, abstract = {Die Kristall- und Molek{\"u}lstrukturen der Akarizide Chlortrineophylstannan (Ia), Chlortris[ ( dimethylphenylsilyl)methyl]stannan (tb) und Trineophyl(1,2,4-triazol-1- yl)stannan-hemihydrat (2a · 0.5H\(_2\)0) wurden durch Einkristall-R{\"o}ntgenstrukturanalysen bestimmt. Zu V ergleichszwecken wurde ausserdem die Struktur des 2,5-Dimethyl-2,5-diphenylhexans (Bineophyl, 4) untersucht. Die Kn{\"u}pfung von drei sehr raumerf{\"u}llenden N eophyl-Resten an ein Zinnatom f{\"u}hrt zu einer deutlichen Verzerrung der tetraedrischen Geometrie [ta: C-Sn-C 117.2°, C-Sn-Cl99.7°; 2a·0.5H20: C-Sn-C 116.9° (Mittelwert), C-Sn-N 100.2° (Mittelwert)]. Austausch der zentralen Kohlenstoffatome in den Neophyt-Substituenten von la durch Siliciumatome f{\"u}hrt zu einer Verringerung des Raumbedarfs und dadurch zu einer erkennbaren Angleichung an die tetraedrische Geometrie [lb: C-Sn-C 113.3° (Mittelwert), C-Sn-Cl 105.3° (Mittelwert)].}, subject = {Anorganische Chemie}, language = {de} } @article{PolidoriMassiLambrechtetal.1990, author = {Polidori, C. and Massi, M. and Lambrecht, G. and Mutschler, E. and Tacke, Reinhold and Melchiorre, C.}, title = {Selective antagonists provide evidence that M\(_1\) muscarinic receptors may mediate carbachol-induced drinking in the rat}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-64044}, year = {1990}, abstract = {The present study served to investigate the ability of seven selective muscarinic antagonists to inhibit carbachol-induced drinking in the rat. The muscarinic antagonists were given by intracerebroventricular (i.c.v.) injection 1 min before the i.c.v. injection of carbachol (1 \(\mu\)g/rat). The M\(_2\) antagonist, methoctramine, was inactive up to 80.3 nmol/rat. The M\(_3\) antagonist, p-fluoro-hexahydro-sila-difenidol, elicited a modest (42\%) but statistically significant inhibition of drinking only at 80 nmol/rat. On the other band, the selective M\(_1\) antagonists, (R)-trihexyphenidyl, o-methoxy-sila-hexocyclium and pirenzepine, produced a marked and dose-dependent inhibition of carbachol-induced drinking, their 1050 values being 0.51. 7.36 and 9.31 nmoljrat. Also the M\(_1\)/M\(_3\) antagonists, 4-diphenylacetoxy-Nmethylpiperidine methiodide and hexahydro-sila-difen.idol, were potent inhibitors of carbachol-induced drinking, their ID\(_50\) values (0.28 and 11.09 nmoljrat) being related to their pA\(_2\) values for M1 receptors in rabbi t vas deferens. These data suggest that carbachol-induced drinking may be mediated by activation of muscarinic M\(_1\) receptors.}, subject = {Anorganische Chemie}, language = {en} } @article{DoerjeWessLambrechtetal.1991, author = {D{\"o}rje, F. and Wess, J. and Lambrecht, G. and Tacke, Reinhold and Mutschler, E. and Brann, M. R.}, title = {Antagonist binding profiles of five cloned human muscarinic receptor subtypes}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-64113}, year = {1991}, abstract = {A variety of muscarinic antagonists are currently used as tools to pharmacologically subclassify muscarinic receptors into M\(_1\), M\(_2\) and M\(_3\) subtypes. ln the present study I we have determined the affinity proflies of several of these antagonists at five cloned human muscarinic receptors (m1-m5) stably expressed in Chinesehamster ovary cells (CHO-K1). At all five receptorsl the (R)-enantiomers of trihexyphenidyl and hexbutinol displayed considerably higher affinities (up to 525-fold) than their corresponding (S)-isomers. The stereoselectivity ratios [inhibition constant( S)/inhibition constant(R)] for both pairs of enantiomers were lowest at m2 receptors, suggesting that less stringent configurational demands are made by this receptor subtype. The "M\(_1\)-selective" antagonist (R)-trihexyphenidyl displayed high affinities for m1 and m4 receptors. The "M\(_2\)-selective" antagonists himbacinel (±}-5, 11-dihydro-11-1[(2-[(dipropylamino)methyl]-1- piperidinyllethyl)amino]carbonyii-6H-pyrido(213-b)(1 ~4)benzodiazepine- 6-one (AF-DX 384)1 11-(14-[4-(diethylamino)butyl)-1-piperidinyll acetyl)-5~ 11-dihydro-6H-pyrido(2~3-b) (1~4)benzodiazepine-6-one (AQ-RA 741) and (+K11-(12-[(diethylamino)methyl]-1-piperidinyll acetyl)-5~ 11-di-hydro-6H-pyrido(2~3-b)(1,4)benzodiazepine-6-one (AF-OX 250; the (+)-enantiomer of AF-DX 116] exhibited high affinities for m2 and m41 intermediate affinities for m1 and m3 and low affinities for m5 receptors. This selectivity profile was most prominent for AQ-RA 7 41 I which displayed 195- and 129-fold higher affinities for m2 and m4 receptors than for mS receptors. The "M\(_3\)-selective" antagonist (±)-p-fluoro-hexahydro-sila-difenidol hydrochloride (pFHHsiD) exhibited high affinity for m1 I m3 and m4 receptors. 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP) bound with up to 7 -fold higher affinities to m1 I m31 m4 and m5 receptors than to m2 receptors. Although none of the tested antagonists showed more than 2-fold selectivity for one subtype over all other subtypes, each receptor displayed a unique antagonist binding profile.}, subject = {Anorganische Chemie}, language = {en} } @article{TackeWiesenbergerBeckeretal.1992, author = {Tacke, Reinhold and Wiesenberger, F. and Becker, B. and Rohr-Aehle, R. and Schneider, P. B. and Ulbrich, U. and Sarge, S. M. and Cammenga, H. K. and Koslowski, T. and Niessen, W. von}, title = {Ester von (Hydroxymethyl)diorganylsilanen: Synthese und thermisch induzierte Umlagerung}, url = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-64188}, year = {1992}, abstract = {Twenty silanes of the type R\(^1\)R\(^2\)Si(H)CH\(_2\)OR\(^3\) (A) were syn- and entropy of activation) of these reactions were studied by thesized {R\(^1\), R\(^2\) = Me, Ph, 1-naphthyl, PhCH\(_2\), Me\(_3\)SiCH\(_2\); OR\(^3\) means of d{\"u}ferential scanning calorimetry (DSC). In addition, = OC(O)Me, OC(O)Ph, OC(O)CF\(_3\) , OS(0)\(_2\)CF\(_3\), OP(O)Ph\(_2\), the kinetics of all reactions were investigated by 1H-NMR OC(O)Cl, and studied for their thermal behaviour. The silanes spectroscopy. The transition state of the rearrangement was A undergo a thermally induced rearrangement to give the investigated by an ab initio study based on the model comcorresponding silanes R\(^1\)R\(^2\)Si(OR\(^3\))Me (B). For compounds with pound H\(_3\)SiCH\(_2\)OC(O)H (-> MeH\(_2\)SiOC(O)H]. The theoretical OR3 = OC(O)Cl, an additional decarboxylation takes place to data and the experimentally obtained energetic and kinetic yield the chlorosilanes R1R2Si(Cl)Me. Except for the deriva- data are discussed in terms of mechanistic aspects of the retives with OR\(^3\) = OC(O)Cl, the energetic (reaction enthalpy) arrangement reaction A -> B. and kinetic data (reaction order, frequency factor, enthalpy ...}, subject = {Anorganische Chemie}, language = {de} }