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

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

Advances in Endogenous and Exogenous Opioids comprises the complaints of the overseas Narcotic learn convention (Satellite Symposium of the eighth foreign 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 realizing of endogenous and exogenous opioids and tackled a wide range of issues starting from novel opiate binding websites selective for benzomorphan medicines to the purification of opioid receptors and sequellae of receptor binding.

Comprised of 156 chapters, this e-book 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 method; and houses of the solubilized opiate receptor from human placenta. next chapters discover the biosynthesis of opioid peptides in addition to their localization, unlock, and degradation; physiological and pharmacological activities of opioids; and using analgesia in acupuncture. result of behavioral and scientific stories of endogenous and exogenous opioids also are awarded, and the structure-activity relationships of opioids are examined.

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

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Goldstein, A. et al. (1979) Proc. NatT. Acad. , 7£, 6666-6670. Chang, K-J. (1979) Mol. , 16, 91-104. Chang, K-J. and Cuatrecasas P. (T979) J . Biol. , 254, 2610-2618. Supported by NIDA (DA 01207). , Tokyo DIFFERENTIAL EFFECTS OF ISOMERS OF OPIOID ANTAGONISTS UPON y-, K- and 6 AGONIST ANALGESIA: COMPARISON WITH OXOTREMORINE. M. E. Sewell Division of Pharmacology, The Welsh School of Pharmacy, UWIST, Cardiff, Wales CF1 3 Nil SUMMARY The narcotic antagonists Mr-1452 and Mr-2266 (but not their (+)-isomers Mr1453 and Mr-2267) antagonized morphine (y), BW 180-C (6) and ethylketocyclazocine (EKC) (K) analgesia in mice whilst the reverse was the case for oxotremorine (OTMN) analgesia.

Effects of various doses of benzomorphan antagonists on the analgesic activity of submaximal doses of morphine (M), BW 180-C (B), EKC (E) and OTMN (0) in the tail immersion test. 01 (for groups of 8-10). Table 1. Comparative doses producing 50% of the maximum possible anti-nociceptive effect in presence or absence of antagonist. ) MPE50 a t 3 0 m i n P o s t d o s e (95^ Confi. 18) 40 (-) antagonists, whilst OTMN was antagonized only by (+) antagonists (Table 1 ) . DISCUSSION The present results indicate that OTMN-induced analgesia in mice is antagon­ ized stereospecifically by the (+) isomers of narcotic antagonists.

Med. Chem. 21, 598. , Tokyo SPECIFIC OPIATE BINDING SITES IN HUMAN PLACENTA A. Valette, G. Porthe", Y. Audigier", G. Pontonnier and J. Cros" INSERM, U. 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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