Advances in Endogenous and Exogenous Opioids. Proceedings of by H. Takagi, Hiroshi Takagi, Eric J. Simon

By H. Takagi, Hiroshi Takagi, Eric J. Simon

Advances in Endogenous and Exogenous Opioids comprises the court cases of the overseas Narcotic examine convention (Satellite Symposium of the eighth overseas Congress of Pharmacology) held in Kyoto, Japan on July 26-30, 1981. The convention supplied a discussion board for discussing advances which were made within the knowing of endogenous and exogenous opioids and tackled a big selection of issues starting from novel opiate binding websites selective for benzomorphan medicinal drugs to the purification of opioid receptors and sequellae of receptor binding.

Comprised of 156 chapters, this publication starts off with an research of the interplay of opioid peptides and alkaloid opiates with mu-, delta-, and kappa-binding websites. The reader is then systematically brought to biochemical facts for kappa and sigma opiate receptors; the motion of morphine and oxymorphone as partial agonists at the field-stimulated rat vas deferens; mechanisms of supersensitivity within the enkephalinergic process; and houses of the solubilized opiate receptor from human placenta. next chapters discover the biosynthesis of opioid peptides in addition to their localization, free up, and degradation; physiological and pharmacological activities of opioids; and using analgesia in acupuncture. result of behavioral and medical experiences of endogenous and exogenous opioids also are offered, and the structure-activity relationships of opioids are examined.

This monograph can be of curiosity to scholars, practitioners, and researchers within the fields of psychiatry and pharmacology.

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Extra resources for Advances in Endogenous and Exogenous Opioids. Proceedings of the International Narcotic Research Conference (Satellite Symposium of the 8th International Congress of Pharmacology) Held in Kyoto, Japan on July 26–30, 1981

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METHODS Male ICI albino mice (18-22 grams) were used. determined in (a) the hot plate test Nociceptive sensitivity was and (b) the tail immersion test . In (a) antinociceptive activity was calculated as the % maximal possible effect (% MPE) and MPE50s with their 95% confidence limits were determined according to the method of Pedigo et al. e. 01 level. RESULTS Thirty minute pretreatment with various doses of either Mr-1452 or Mr-2266 39 antagonized opioid analgesia in the tail immersion test contrasting with OTMN which was only antagonized by Mr-1453 dose dependently, Mr-2267 antagonism being biphasic (Fig.

For pharmacological studies 6-OHDA or vehicle-treated Pg were challenged with opiates 5 days after treatment. Pg from 4 animals were excised 1 hour after opiate administration, pooled and assayed for monoamine content by spectrofluorimetry 5 ' 6 . Radiolabelled opiate binding to Pg from vehicle or 6- OHDA-treated animals was assayed as described 7 ; data are means of 5 experiments. RESULTS Histofluorescence photomicroscopy of the cortex region of untreated M. edulis 48 Pg revealed the presence of yellow- and green-fluorescing nerve cell bodies, which correspond to serotonin- and catecholamine-containing neurons, respectively^.

168 Hopital La Grave, Toulouse and "CNRS Laboratoire de Pharmacologie et de Toxicologie Fondamentales 205. route de Narbonne, 31 078 TOULOUSE Cedex, France. SUMMARY Human placenta contains s p e c i f i c binding sites for 3 H-etorphine and 3,H-ethylketocyclazocine, which pharmacological characteristics correspond to the kappa receptors. These opiate binding s i t e s , s p e c i f i c a l l y found in the human species are located on brush border membranes of the syncytiotrophoblaste and t h e i r number increases between the 2 and the 5 month of gestation.

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