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Opioid antagonists kappa-receptor selective

Further studies in mouse vas deferens indicated that DPI-3290 is also active at mu opioid receptors. The intrinsic activity of DPI-3290 at mu opioid receptors was determined in the presence of the highly selective delta opioid receptor antagonist TIPP (H-Tyr-Tic-Phe-Phe-OH) (3 pM) and the selective kappa opioid receptor antagonist nor-BNI (15 nM). Under these conditions, DPI-3290 again caused concentration-dependent inhibition of muscle contraction with a corresponding IC50 value of 6.2 2.0 nM. Although far less potent at kappa opioid receptors in comparison to its intrinsic activity at mu... [Pg.236]

Interestingly, morphine is primarily considered to have selective effects on the mu opioid receptor for its analgesic effects however, there is also evidence that it possesses effects on delta or kappa opioid receptors and that crosstalk can occur between mu and delta opioid receptors [44]. To test the hypothesis that the cardioprotective effects of IPC and morphine were acting via a delta opioid receptor, Schultz et al. [45] administered the selective delta receptor antagonist naltrindole to rats prior to IPC or morphine infusion. In both instances, the cardioprotective effects of morphine and IPC were completely abolished at a dose of naltrindole that had no effect by itself on infarct size in nonpreconditioned rat hearts. These data clearly suggest that both IPC and morphine are exerting their cardioprotective effects via the delta opioid receptor in the intact rat heart. [Pg.456]

Manzanares J, Lookingland KJ, LaVinge SD, Moore KE (1991c) Activation of tuberohypophysial dopamine neurons following intracerebroventricular administration of the selective kappa opioid receptor antagonist nor-binaltorphimine. Life Sci 5 1143-1149. [Pg.512]

Portoghese, P.S., Lipkowski, A.W., Takemori, A.E., 1987. Binaltor-phimine and norbinaltorphimine, potent and selective kappa opioid receptor antagonists. Life Sci. 40, 1287-1292. [Pg.274]

Negus SS, Henriksen SJ, Mattox A, Pasternak GW, Portoghese PS, Takemori AE, Weinger MB, Koob GF. (1993). Effect of antagonists selective for mu, delta, and kappa opioid receptors on the reinforcing effects of heroin in rats. J Pharmacol Exp Ther. 265(3) 1245-52. [Pg.527]

The biochemical and pharmacological properties of the kappa receptor and the differences between the kappa, mu and delta receptors have been reviewed elsewhere. The reader is directed to the opioid review articles by Rees and Hunter (1990) [4], Casy (1989) [3] and Leslie (1987) [10] and also to two shorter reviews which deal specifically with kappa agonists the review by Horwell published in 1988 entitled Kappa Opioid Analgesics [8] and the review by Millan in 1990 on kappa opioid receptors and analgesia [9]. An account of the medicinal chemistry of selective opioid agonists and antagonists was published in 1990 by Zimmerman and Leander [5]. [Pg.113]

The direct effects opioid and opioidlike peptides exhibit on cells of the immune system is both varied and, in some instances, contradictory, depending on which receptor subtype is being studied. Mu and kappa receptors generally affect immunofunction in a suppressive manner, where delta receptors tend to express immunostimulation [82-85]. However, selected delta antagonists have shown to elicit suppressive effects on B-cell proliferation, NK cell activity, and T-helper cell cytokine production [86]. The alteration of leukocyte function via opioid receptors will be discussed highlighting specific cell subtype immunomodulation. Endorphin shows a inhibitory effect on splenocyte proliferation through central and peripheral autocrine/paracrine pathways [87]. [Pg.390]

Menthol is a cyclic alcohol present in the volatile oil of several species of mint such as Mentha piperita and Mentha aevensis. It is responsible for the typical minty smell and flavour. (-)-Menthol produced a dose-dependent increase in the pain threshold in the mouse hot-plate and abdominal constriction tests. The antinociceptive effects of (-)-menthol were antagonized by the unselective opioid antagonist naloxone and by the selective kappa-antagonist nor-NBI. Thus, menthol has analgesic properties mediated by selective activation of kappa-opioid receptors. [Pg.207]

In the search for kappa (k) opioid antagonists only one drug substance gained cognizance, which is ( ) nor-binaltorphimine, and it showed fairly good selectivity for the kappa receptors. ... [Pg.309]


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See also in sourсe #XX -- [ Pg.6 , Pg.348 , Pg.365 , Pg.366 ]




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Kappa

Kappa opioids

Kappa receptors

Kappa-opioid receptors

Kappa-selective opioid receptor

Opioid antagonists

Opioid receptor antagonists

Opioid receptors

Opioids kappa receptor

Opioids receptors

Selective antagonists

Selective receptors

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