Pharmacological examination

The compounds in a suitable solvent were subcutaneously in-jected into mice. Methyl fluoroacetate was always injected, under the same conditions, into a batch of mice as a control. The y -carbon atom in y -2 fluoroethoxypropionic acid and in y 3 fluoropropoxypropionic acid is linked to the ether oxygen atom, and if/ -oxidation of these compounds takes place in vivo, the hydrogen carbonate of the fluoro alcohol is formed. One would expect this to have approximately the same toxicity as the alcohol itself, since the latter would be produced either by hydrolysis or by ehmination of carbon dioxide  

This was verified by showing that ethyl 2 fluoroethyl carbonate was as toxic as 2 fluoroethyl alcohol. Furthermore, we found that y 2-fluoroethoxypropionic acid was indeed toxic, whereas y 3 fluoropropoxypropionic acid was non-toxic. (3 Fluoro-propanol is itself non-toxic.) 

The actual l.d. 50 for ff 2 fluoroethoxypropionic acid, how-ever, was about 70 mg./kg. and was therefore considerably less than that for fluoroethyl alcohol, whereas the nitrile of the acid showed a toxicity (l.d. 50, 10-20 mg./kg.) of the same order as that of the alcohol. The cause of this difference may be due to different rates of absorption. 2-3 -Fluoropropoxyethyl cyanide was non-toxic in accordance with expectation. 

In this connexion ethyl 2 cyanoethyl ether, EtO-[CH2]2 CN, was tested and found to be relatively non-toxic, showing that the toxicity of the fluorine analogue was caused ultimately by the presence of the fluorine atom (as fluoroethoxyl) and not to any extent by another part of the molecule. 

2 Fluoro- and 2 hydroxy 2 2 fluoroethoxydiethyl ether were both toxic the former had a l.d. 50 of 15-20 mg./kg. and the latter of 30-40 mg./kg. If the former is readily oxidized to the corresponding acid in the animal body, then we should ex-pect it to be non-toxic in view of the non-toxicity of ethyl 2-fluoroethoxyacetate referred to above. It must be concluded then that the ether alcohols exert some toxic action per se. Ethylene glycol monoethyl ether, was examined physiologically but was found to be non-toxic, showing that the activity of 2-fluoro-2 -hydroxydiethyl ether was again closely associated with the 2-fluoroethoxy group in the molecule. 

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The crude drug, Adhatoda vasica, is used in India as a remedy for asthma. According to Chopra, vasicine produces broncho-dilation and might be used clinically as an expectorant. A detailed pharmacological examination of peganine in comparison with harmine has been made by Tutaev and Makarova. ... 

As already stated, the number of substances made by chemists for pharmacological examination as possible sympathomimetic amines is enormous and the literature voluminous. Fortunately the latter has been reviewed from time to time, and most recently in the symposium in which Hartung dealt with the correlation of structure and pharmacological action in )3-phenylethylamine derivatives, which includes the more impor-... 

Katzung BG, Trevor AJ. Pharmacology, Examination Board Review, Prentice-HiU International, Englewood Chffs, NJ, 1995. 

An important related educational resource is Katzung Trevor s Pharmacology Examination Board Review, eighth edition (Trevor A3, Katzung BG, Masters SB McGraw-Hill, 2008). This book provides a succinct review of pharmacology with over one thousand... 

Drug Interactions Analysis and Management (quarterly). Wolters Kluwer Publications, 111 Westport Plaza, Suite 300, St Louis, MO 63146. Pharmacology Examination Board Review, 7th ed. McGraw-Hill Companies, Inc, 2 Penn Plaza 12th Floor, New York, NY 10121-2298. Symposium Allosterism and collateral efficacy. TIPS 2007 28(8) entire issue. 

Reproduced, with permission, from Trevor AT, Katzung BG, Masters SB Pharmacology Examination Board Review, 6th ed. McGraw-Hill, 2002.)... 

The earliest attempts to develop a non-dependence-inducing morphine derivative resulted in the preparation of heroin (3,6-diacetylmorphine) by acetylation of morphine (Wright, 1874, Dreser, 1898). The potency of heroin was soon recognized. It underwent more investigation than any other product of the time, and was introduced into clinical medicine in 1898. Reports of its reduced respiratory depression and dependence liability were soon shown to be unfounded, but its analgesic effects in animals and man (twice morphine) were confirmed. Pharmacological examination of acyl derivatives of morphine showed that... 

Students who wish to review the field of pharmacology in preparation for an examination are referred to Pharmacology Examination and Board Review, by Trevor, Katzung, and Masters (McGraw-Hill, 2002) or USMLE Road Map Pharmacology, by Katzung and Trevor (McGraw-Hill, 2003). 

Pharmacology Examination Board Review, 6th ed McGraw-Hill Companies, Inc 2 Penn Plaza 12th Floor New York, NY 10121 -2298... 

Antiviral actions of purine and pyrimidine analogs. Acyclovir and ganciclovir (top) are phosphorylated first by viral kinase to the monophosphate. This intermediate and the drugs shown on the left are then phosphorylated by host cell kinases to the nucleotide analogs that inhibit viral replication. (Modified and reproduced, with permission, from Trevor AT, Katzung BG, Masters SM Pharmacology Examination Board Review, 6th ed. McGraw-Hill, 2002.)... 

Antibacterial agents linked to polymers have been investigated by various teams. In this case pharmacological examination is easier, since screening tests are often sufficient. However, the results of such in vitro tests are not always transferable to in two-systems and are not always reproducible. 

DNLM 1. Pharmacology—examination questions. 2. Pharmacology—outlines. QV 18.2 M995p 1997] RM301.14.P47 1997 615. 1 076—dc20 DNLM/DLC... 

Toxicological and pharmacological examinations of Sala nandra alkaloids have been made by Faust (18) and later by Gessner (19-23). Gessner also found the secretion to contain hemolytically active peptides in addition to the alkaloids. 

Ellis, J.L., Undem, B.J., Kays, J.S. etal. (1993). Pharmacological examination of receptors mediating contractile responses to tachykinins in airways isolated from human, guinea-pig and hamster. J. Pharmacol. Exp. Ther. 267, 95-101. 

Katzung Trevor s Pharmacology Examination Board Review, Sixth Edition... 

Brownlee, G. 1940. A pharmacological examination of cineole and pheUandrone. Quart. J. Pharm. Pharmacol. 13 130-137. Chennoufi, R., J. Morizue, H. Richard, and F. Sandret. 1980. Etude des huiUes essentieUes d Eucalyptus globulus au Maroc. Riv. Ital. 62 353-357. 

Magistretti, M.J. 1980. Remarks on the pharmacological examination of plant extracts. Fitoterapia 51 67-79. 

The present review summarizes the work of the last fifty years in the field of the synthesis of Erythrina alkaloids and structurally related compounds. Their unique structure has attracted the attention of the synthesis chemists over a period of more than half a century until now. The numerous efforts devoted to the construction of the tetracyclic spiroamine framework have certainly led to original and impressive results, but with regard to today s standard and especially to an adequate supply of the promising compounds for a systematic pharmacological examination the total efficiency of their preparation yet leaves wishes in many cases. 

Cardiovascular Pharmacology. Cardiovascular pharmacology examines the effects of drugs on the heart and vascular system, as well as on other body... 

B. mtmobasiana Stapf. (a false iboga, p. 768). Pharmacological examination of an extract. (Raymond-Hamet. )... 

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