Prostaglandin pharmacological properties

The dioxopyrazolines are also acidic because of their enolic group (4,4-disubstituted analogues are inactive) and a recent example azapropazone (apazone) (184) inhibits prostaglandin synthesis. Its pharmacological properties are like those of phenylbutazone and it is also uricosuric. Anti-inflammatory 1,2-benzothiazine 1,1-dioxides such as piroxicam (185 R = 2-pyridyl) also have an acidic enolic group whose anion can be stabilized by... 

Despite their fascinating pharmacological properties, prostaglandins are difficult drugs to administer because, in addition to their natural scarcity, they are rapidly inactivated by enzymatic degradation and interact nonselectively with tissues and cells. Despite these difficulties, biosynthetic production of PGs has not met increasing demand. Biosyn-... 

The prostacyclins have important pharmacological properties. A synthesis of PGi (486) from the prostaglandin F2a (487) has been reported by Corey (77JA2006). 

Arachidonic acid ethanolamide (anandamide) and similar compounds are constituents of the brain. Anandamide and certain of the compounds similar with same, bind to the cannabinoid receptor. The binding of the ananamide to the cannabinoid receptor is similar to the binding of A9-tetrahydrocannabinol. There exist in the body many mediators, which are derivatives of arachidonic acid, such as prostaglandins and leukotrienes, which are present as large families of related compounds. Certain of these do not bind to the cannabinoid receptor, and it was one of the aims of the present invention to provide and identify compounds which have pharmacological properties similar to the properties of anandamide. 

There are however a very large number of prostaglandins and these show difiiering pharmacological properties. They have therefore different applications in health care. These compounds are, however, cmly produced in very small quantities by natural systems. Therefore a variety of strat es have been develop to produce d ese biologjcal con unds in larger quantities in mtro. This usually involves a mixture of chemical and... 

Table 36.2. Pharmacological Properties of Prostaglandins, Thromboxane, and Prostacyclin...

The prostaglandins are a new family of acidic lipids which are present in many, if not all, mammalian tissues and which have a wide variety of striking pharmacological properties both in vivo and in vitro. Individual prostaglandins in exceedingly small doses may stimulate or relax the uterus and Fallopian tubes, stimulate intestinal smooth muscle, constrict the pupil, dilate peripheral and coronary arteries, constrict veins, constrict nasal and placental blood-vessels, excite or... 

The colorless oil is an important unsaturated (all double bonds are cisj, essential (->fats and oils) fatty acid, which can be gained from - fish oil. It is a predecessor of - prostaglandin and - thromboxane, which show many important pharmacological properties. E.-containing medical preparations are of economic significance, especially in Japan. 

In the preceding chapters, the synaptic pharmacology of those substances clearly established as NTs in the CNS, i.e. glutamate, GABA, ACh, NA, DA, 5-HT and certain peptides, has been discussed in some detail. There are other substances found in the CNS that could have a minor transmitter role, e.g. ATP, histamine and adrenaline, while still others that cannot claim such a property but clearly modify CNS function in some way, e.g. steroids, prostaglandins and nitric oxide. We will consider each of them in what we hope is appropriate detail. 

The enteropooling assay in rats has been developed by Robert et al. (1976) to test the diarrhoeic property of prostaglandins for prediction of this clinically relevant side effect of several synthetic prostaglandins. This method can also be used for the safety pharmacological assessment of candidate compounds on their side effect potential to induce diarrhoea. 

Chintakunta VK, Akella V, Vedula MS et aL (2002) 3-0-Substituted benzyl pyrazidone derivatives as COX inhibitors. Eur J Med Chem 37 339-347 Coleman RA, Smith WL, Narumiya S (1994) VIII. International union of pharmacology classification of prostanoid receptors Properties, distribution, and structure of the receptors and their subtypes. Pharmacol Rev 46 205-229 Copeland RA, Williams JM, Giannaras J et al. (1994) Mechanism of selective inhibition of the inducible isoform of prostaglandin G/H synthase. Proc Natl Acad Sd USA 91 11202-11206... 

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