Spelling suggestions: "subject:"antagonist""
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Pyroglutamic acid and 6 oxopipecolic acid as chiral synthons for compounds of medicinal interestAhmed, Omar January 2003 (has links)
Prevention of the neurotoxic effect that excess glutamic acid has on its receptors can lead to the treatment of a number of neurodegenerative diseases and pathological conditions. Developments of new methods for the stereospecific synthesis of novel amino acids will allow identification of compounds which might be effective at these receptors to be prepared. (2S)-Pyroglutamic acid was used as a chiral template for the synthesis of a key aldehyde for use in a novel synthesis of glutamate antagonists. Subsequent ring transformation ('ring-switching') reactions using bisnucleophiles then afforded a number of homochiral pyridazines that, when deprotected and oxidized, would possess the structural requirements of glutamate antagonists. A number of other routes requiring protection of the aldehyde were studied with the aim of synthesising a library of substituted homochiral pyridazines. Ring transformations involving an a, ß-unsaturated lactam with methyl hydrazine were also briefly studied, furnishing chiral pyrazolidin-3-ones with potential for glutamate receptor activity. The second area of research involved investigation of a stereoselective route to 5- alkylated 6-oxopipecolates from a 5-substituted enaminone. Initial attempts to prepare the enaminone tert-butyl ester from tert-butyl (2S)-N-tert-butoxycarbonyl-6- oxopipecolate were unsuccessful, but the enaminone methyl ester was eventually successfully prepared from methyl (2S)-N-tert-butoxycarbonyl-6-oxopipecolate. This enaminone was reacted with a number of Grignard reagents to afford a range of 5- alkylidene derivatives which were all (E)-isomers. Catalytic reduction of these was stereoselective and so an effective route to methyl (2S, 5S)-5-alkyl-6-oxopipecolates has been developed. A route involving alkylation of methyl (2S)-N-tert-butoxycarbonyl-6- oxopipecolate followed by enhancement of stereoselectivity using a hindered proton source was also investigated.
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PHYSIOLOGICAL CHARACTERIZATION OF PINEAL ANTIGONADOTROPINWray, Mary Jane Matthews January 1978 (has links)
No description available.
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Pre- and postjunctional effects of neuromuscular blocking drugsGibb, A. J. January 1983 (has links)
No description available.
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Effect of Calcium Channel Antagonists and Other Agents on Olfactory ReceptionRosick, Edward R. (Edward Rudolph) 08 1900 (has links)
The role of Ca++ in olfactory responses was investigated with inorganic and organic calcium channel antagonists. Electrophysiological responses to odorants were recorded from frog olfactory mucosa before and after aerosol application of different agents. Electroolfactogram responses were blocked by certain inorganic ions with the order of effectiveness Zn++ >Ln+++>Cd++>Ca++>Co++>Sr++>Mg++. Ba++ potentiated olfactory responses, and is known to potentiate calcium channel-mediated responses in other tissues. Certain local anesthetics which are thought to act through calcium channel blockade were inhibitory to olfactory responses, with the order of effectiveness being dibucaine>tetracaine>procaine. These data support the idea that Ca++ is involved in olfaction, perhaps acting as a current carrier and/or a second messenger. Preliminary experiments on channel localization were performed using a silicon-labeled amine. Attempts to localize the silicon label were inconclusive, although silicon was detected in the olfactory tissue.
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Molecular determinants of picrotoxin inhibitionErkkila, Brian E. January 2007 (has links) (PDF)
Thesis (Ph. D.)--University of Alabama at Birmingham, 2007. / Title from first page of PDF file (viewed Oct. 13, 2008). Includes bibliographical references.
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Effect of ovine luteinizing hormone antibodies on reproduction in rabbitsQuadri, Syed Kaleemullah. January 1966 (has links)
Call number: LD2668 .T4 1966 Q1 / Master of Science
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Prevalence of gastro-intestinal bleeding in hypertensive patients taking calcium blockers in a regional acute hospital in Hong KongLai, Wing-fu., 賴永富. January 2009 (has links)
published_or_final_version / Pharmacology and Pharmacy / Master / Master of Medical Sciences
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Pharmacological manipulation of aromatic L-amino acid decarboxylase in the ratFisher, Andrew January 1999 (has links)
No description available.
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Factors affecting the pharmacokinetics of nifedipine in humansRashid, T. J. January 1994 (has links)
No description available.
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Intracellular mechanisms of action of cardioprotective agentsHassan, Lobna Mohammed Saber Abdel January 1997 (has links)
No description available.
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