By H. Takagi, Hiroshi Takagi, Eric J. Simon
Advances in Endogenous and Exogenous Opioids comprises the lawsuits of the foreign 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 have been made within the knowing of endogenous and exogenous opioids and tackled a wide range of subject matters starting from novel opiate binding websites selective for benzomorphan medications to the purification of opioid receptors and sequellae of receptor binding.
Comprised of 156 chapters, this booklet starts 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 method; and houses of the solubilized opiate receptor from human placenta. next chapters discover the biosynthesis of opioid peptides in addition to their localization, unencumber, and degradation; physiological and pharmacological activities of opioids; and using analgesia in acupuncture. result of behavioral and scientific reviews 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
SUMMARY Evidences that dynorphin-(l-13) acted as kappa-receptor agonist and that rabbit and dog ileum contained the new type of opiate receptor which was tentatively termed iota receptor, were obtained by the study on effects of opioids on the electrically-evoked contractions of several isolated preparations. INTRODUCTION Enkephalins have been shown to act either on mu or on delta receptor depending on the coexisted opiate-receptor subtype1. It is uncertain, however, whether enkephalins act on delta receptor or not in the rabbit ileum which has been shown to be not sensitive to morphine but sensitive to enkephalins .
Waterfield, A. , Hughes, J. and Kosterlitz, H. W. (1977) Nature, 267. 495-499. Woods, J. , Smith, C. , Medzihradsky, F. and Swain, H. H. (1979) "Mechanisms of Pain and Analgesic Compounds" (ed. Beers, R. F. and Bassett, E. G . ) , p. 429-446, Raven Press, New York. , Tokyo COMPARISON OF H-ETORPHINE AND H-DIPRENORPHINE RECEPTOR BINDING IN VIVO AND IN VITRO M, Kurowski, J. C. Perry and W. A. ) cerebral ste- reospecific high affinity binding jLn vivo was determined in rats using a rapid membrane filtration technique performed immediately after brain homogenization.
1 ) . DISCUSSION 3 It is concluded that the differences of is^ vivo binding between H-diprenor3 + phine and H-etorphine can be resolved by the synergistic effects of Na and 3 3 GPPNHP on H-etorphine, but not H-diprenorphine, binding. Comparison of the etorphine and diprenorphine doses that occupy 50% of the ±n vivo binding sites (^ 50 yg/kg and ^ 12 yg/kg, respectively) with the dose required for half maxi mum pharmacological effect (^ 1 yg/kg and a ^10 yg/kg, respectively) revealed another striking difference between the agonist and the antagonist; etorphine 3 H- analgesia occurs at a receptor occupancy of only 2% of the labeled in vivo etorphine binding sites, while antagonistic effects of diprenorphine occur ap proximately in proportion to its fractional receptor binding.
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 by H. Takagi, Hiroshi Takagi, Eric J. Simon