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Summary Oxotremorine (Ia) and its succinimide analogue (IIa) have been substituted in the pyrrolidine ring with a methyl group in the 2- or 3-positions. The compounds are oxotremorine antagonists. The 2-methyl-substituted enantiomers show stereoselectivity, the S-isomers being the most active. 相似文献
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S. Lindgren Å. Lindquist B. Lindeke U. Svensson B. Karlén R. Dahlbom M. R. Blair Jr 《Cellular and molecular life sciences : CMLS》1970,26(11):1232-1233
Zusammenfassung Eine Anzahl von Antagonisten zu Oxotremorin wurden durch kleine Modifikationen der Struktur des Oxotremorins erhalten. Die aktivste Verbindung, N-(1-Methyl-4-pyrrolidino-2-butinyl)pyrrolidon, ist mehr als sechsmal wirksamer als Atropin und hat eine grössere Spezifizität mit Bezug auf das Zentralnervensystem. 相似文献
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Zusammenfassung Die Stereospezifität der Enzyme des Allantoinabbaus inStreptococcus allantoicus und die optische Drehung der Reaktionsprodukte wurde bestimmt. Allantoinase war aspezifisch, während Allantoate-amidohydrolase ausschliesslich (-)-Ureidoglykolate bildete. Diese Substanz wurde durch (-)-Ureidoglykolase hydrolysiert. 相似文献
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B. Wermuth J. D. B. Münch J. P. von Wartburg 《Cellular and molecular life sciences : CMLS》1979,35(10):1288-1289
Summary Aldehyde reductase from human liver catalyzes the hydrogen transfer from the pro-4R position on the dihydronicotinamide ring of the coenzyme to there face of the carbonyl carbon atom of the substrate. 相似文献
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Zusammenfassung Eine zentrale, nikotinartige Wirkung von Oxotremorin wird am Blutdruck der Ratte beschreiben. 相似文献
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Aldehyde reductase from human liver catalyzes the hydrogen transfer from the pro-4R position on the dihydronicotinamide ring of the coenzyme to the re face of the carbonyl carbon atom of the substrate. 相似文献
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H. Shio P. W. Ramwell N. H. Andersen E. J. Corey 《Cellular and molecular life sciences : CMLS》1970,26(4):355-357
Zusammenfassung Die stereochemischen Voraussetzungen der Prostaglandin-15-Dehydrogenase aus Schweinelunge werden im Hinblick auf die pharmakologische Aktivität anhand einer Reihe synthetischer Prostaglandin E1-Präparate abgeklärt.
This work was supported by grants from the U.S. National Institutes of Health to Harvard University and by O.N.R. and N.I.H. grants to the Worcester Foundation for Experimental Biology. 相似文献
This work was supported by grants from the U.S. National Institutes of Health to Harvard University and by O.N.R. and N.I.H. grants to the Worcester Foundation for Experimental Biology. 相似文献
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Integrin antagonists 总被引:4,自引:0,他引:4
Integrins are a family of cell surface glycoproteins that mediate numerous cell-cell and cell-matrix interactions and are
involved in biological processes such as tissue morphogenesis, leukocyte recirculation and migration, wound healing, blood
clotting and immune response. Aberrant cell adhesion has been implicated in the pathogenesis of several diseases, including
a number of inflammatory disorders such as rheumatoid arthritis, inflammatory bowel disease and asthma, as well as cancer
and coronary heart disease. As such integrins are seen as excellent targets for the development of therapeutic agents. This
report begins with an examination of the structure of integrin molecules and their ligands and then goes on to review the
current state of development of antiintegrin antagonists.
Received 13 April 1999; received after revision 28 May 1999; accepted 28 May 1999 相似文献
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Effects of vasopressin via V1a- and V2-receptors are closely implicated in a variety of water-retaining diseases and cardiovascular
diseases, including heart failure, hyponatraemia, hypertension, renal diseases, syndrome of inappropriate antidiuretic hormone
secretion, cirrhosis and ocular hypertension. As vasopressin receptors are found in many different tissues, vasopressin antagonists
may benefit the treatment of disorders such as cerebral ischaemia and stroke, Raynaud’s disease, dysmenorrhoea and tocolytic
treatment. V1b selective vasopressin antagonists are discussed in terms of their usefulness in the treatment of emotional
and psychiatric disorders. The vaptans are vasopressin receptor antagonists with V1a (relcovaptan) or V2 (tolvaptan, lixivaptan)
selectivity or non-selective activity (conivaptan) which may be advantageous in some disorders. The V1a/V2 non-selective vasopressin
antagonist conivaptan is the first vaptan which is approved by the FDA for the treatment of euvolaemic hyponatraemia.
Received 3 February 2006; received after revision 16 March 2006; accepted 26 April 2006 相似文献
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D. W. Graham J. E. Brown W. T. Ashton R. D. Brown E. F. Rogers 《Cellular and molecular life sciences : CMLS》1977,33(10):1274-1276
Summary 4 types of riboflavine antagonists have broad-spectrum activity in poultry coccidiosis. 5-Deazariboflavine is most effective. 10-Benzyl analogs of riboflavine control intestinal species of coccidia. 相似文献
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Peter C. Waldmeier Rainer Ortmann Serge Bischoff 《Cellular and molecular life sciences : CMLS》1982,38(10):1168-1176
Summary The effects on dopamine (DA) metabolism, on3H-spiperone binding and on amphetamine-induced stereotypies of a variety of drugs with different actions on alpha1-and alpha2-noradrenergic (NA) receptors have been investigated.The preferential alpha2-antagonists yohimbine, rauwolscine, piperoxane and esproquin as well as the preferential alpha1-antagonists corynanthine and WB4101 increased homovanillic acid (HVA) and 3,4-dihydroxyphenylacetic acid (DOPAC) in the rat striatum, mesolimbic area, and cortex. Prazosine and clonidine tended to reduce HVA and DOPAC. The preferential alpha2-antagonists, tolazoline and RX-781094A, had no measurable effects on DA metabolism even at high doses.Those compounds which in comparable doses increased DA metabolism inhibited3H-spiperone binding in the hippocampus. The effects in the striatum and cortex were smaller and did not show a relation to those in hippocampus or on DA metabolism. Only the yohimbine alkaloids antagonized amphetamine-induced stereotypies.The results suggest that the effects on DA metabolism at least of yohimbine, rauwolscine, and corynanthine are related to their intrinsic antidopaminergic properties. The same might be true, although with a lesser degree of certainty, for piperoxane, esproquin, and WB4101.Since many of the tested compounds possessing alpha-antagonistic properties interacted with the DA system, a close molecular relationship between alpha-noradrenergic and DA receptors might be anticipated. The preference of these compounds for the hippocampal subtype of DA receptors might indicate a particular role of the latter in the regulation of DA metabolism. On the other hand, the antagonism against haloperidol's enhancing effect on DA metabolism by clonidine suggests a modulatory NA influence on DA transmission. The observation that clonidine reduced the effects of yohimbine and piperoxane to a lesser degree than that of haloperidol, is in agreement with this notion.Part of this work has been presented at the 13th Meeting of the Union of Swiss Societies of Experimental Biology, Lausanne, March 26/27. 1981 (for abstract see Waldmeier and Bischoff, 1981). 相似文献