Pharmacological uses

Hydrolases represent a significant class of therapeutic enzymes [Enzyme Commission (EC) 3.1—3.11] (14) (Table 1). Another group of enzymes with pharmacological uses has budt-ia cofactors, eg, in the form of pyridoxal phosphate, flavin nucleotides, or zinc (15). The synthases, and other multisubstrate enzymes that require high energy phosphates, are seldom available for use as dmgs because the required co-substrates are either absent from the extracellular space or are present ia prohibitively low coaceatratioas. 

Pharmacologically useful isoxazoles (B-82MI41600) include antibacterial sulfonamides (614), (615) and (616), semisynthetic penicillins (617), (618), (619) and (620), semisynthetic cephalosporin (621), anabolic steroid (622), the monoamine oxidase inhibitor (623) (used in psychotherapy), antiinflammatory agent (624) and antitumor agent (625). 

Thiirane is more bactericidal than oxirane, and derivatives of 2-mei captomethylthiirane inhibit tuberculosis. The following pharmacological uses have been reported for compounds derived from thiirane derivatives gold complexes of the adducts of diethylphosphine and thiirane (antiarthritic), adducts of thiiranes and malononitrile (antibacterial, blood vessel dilators, muscle relaxants, sedatives), thermolysis products of thiirane 1-oxides and adducts of thiirane 1-oxides with sulfenyl chlorides (antibacterial), adducts of 2,3-diarylthiirene 1,1-dioxides with ynamines (antibacterial, parasiticidal), adducts of 2,3-diarylthiirene 1,1-dioxides with enamines (antifertility), adducts of p-aminophenylacetic esters with thiirane (immunosuppressants), adducts of amines and thiiranes (radioprotective drugs). 

Yu JX, Kodibagkar VD, Cui WN, Mason RP (2005) F-19 a versatile reporter for non-invasive physiology and pharmacology using magnetic resonance. Curr Med Chem 12 819-848... 

The first report on the anticancer properties of ruthenium was published in 1976 when the Ru(III) compound /ac-[RuC13(NH3)3] (Fig. 11) was found to induce filamentous growth of Escherichia coli at concentrations comparable to those at which cisplatin generates similar effects (49). This Ru(III) complex and related compounds such as cis-[RuCl2(NH3)4]Cl illustrated the potential anticancer activity of ruthenium complexes, but insolubility prevented further pharmacological use. Since these initial studies, other Ru(III) complexes have been studied for potential anticancer activity, and two compounds, NAMI-A (50) and KP1019 (51), are currently undergoing clinical trials. Remarkably,... 

Green, M.D. (1997). Problems associated with the absence of activity in standard models of safety pharmacology used to assess biological products. Ini. J. Toxicol. 16 33—40. 

Despite their importance in many pharmacological uses and potential applications, solubilities of hydroxypyranones, hydroxypyridinones, and their complexes have not been extensively and systematically investigated and established. This situation contrasts sharply with that for partition coefficients, as will become apparent in the following section. The solubility of maltol in water is approximately 0.1moldm , of ethyl maltol 0.13 mol dm, at 298 K. 1,2-Alkyl-3-hydroxy-4-pyridinones show the expected decrease in water-solubility as the sizes of the alkyl groups increase solubilities - in water at 298 K - of l-aryl-2-methyl-3-hydroxy-4-pyridinones decrease from 9 X 10 mol dm for the 1-phenyl compound through 6 x lO- moldm for l-(4 -tolyl) to 6 x 10 mol dm for l-(4 -re-hexyl-phenyl) (37). 

GHB was hrst synthesized in the laboratory by the French biochemist Henri Lahorit (1914-1995) in 1961. In the succeeding four decades, extensive research has been conducted on the pharmacological uses and effects of GHB. In general, those studies appear to suggest that GHB has some valuable applications in the medical sciences. It functions well as an anesthetic with apparently few or no serious side effects. Based on this research, the drug has been adopted in many parts of the world for use as a general anesthetic, a treatment for narcolepsy and insomnia, a treatment for alcoholism, and an aid in childbirth. 

The continuing interest in the chemistry of the 1,3-oxazines and the related thiazines and pyrimidines may arise in part from their versatile synthetic applicability and their pharmacological usefulness. Although six-membered saturated or partially saturated 1,3-heterocycles and their derivatives fused with a benzene ring have been thoroughly studied since the beginning of the twentieth century, much less attention has been paid to their saturated counterparts, the related cycloalkane-fused bicyclic 1,3-heterocycles. 

When sulfur functional groups and heteroaromatics are combined, an entirely new field of chemistry emerges. Pharmacological uses have expanded for example, introduction of a sulfur atom into nitrogen hetero-... 

Non-Invasive Physiology and Pharmacology Using Magnetic Resonance... 

These modifications make pramlintide soluble and non-self-aggregating and suitable for pharmacologic use. 

Hydrolases represent a significant classes of therapeutic enzymes (Table 11. Another group of enzymes with pharmacological uses has built-in cofactors, c.g.. in the form of pyridoxal phosphate. Ilavin nucleotides, or zinc. 

This approach includes the production and purification of antisense transcripts in vitro and then the introduction of the antisense RNA into cells by microinjection. Compared to the antisense gene approach described above, a major advantage of this method is that a much larger amount of antisense RNA can be introduced into cells. Also, antisense RNA can be injected at a specific time and can therefore result in the transient inhibition of gene expression, which can be used in studies of gene expression at a specific time within a particular window of development. However, as RNAs are extremely sensitive to nuclease degradation, the potential pharmacological uses of antisense RNA are limited. 

This chapter first discusses the physiologic role of the male hormones and the pharmacologic use of natural and synthetic androgens. The physiologic and pharmacologic characteristics of the female hormones are then addressed. As these discussions indicate, there are several aspects of male and female hormones that should concern physical therapists and occupational therapists. Rehabilitation patients may use these agents for approved purposes, for example, female hormones as contraceptives. These agents may also be... 

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