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The antinociceptive properties of morphine-6 beta-glucuronide (M6G) and morphine (oral, i.c.v. and s.c.) were examined in two tests involving different nociceptive stimuli [i.e., cutaneous-thermal (tail-flick) and chemical-visceral (acetic acid-writhing)] in both naive and chronically treated mice. Twenty min after i.c.v. injection, M6G was 47 and 360 times(More)
Ajoene, a garlic stable oil-soluble sulfur rich compound was generally isolated as a mixture of two isomers [(E, Z)-4,5,9-trithiadodeca-1,6,11-triene-9-oxide]. It has been described essentially as a potent inhibitor of platelet aggregation in vitro and in vivo. The antiproliferative effects of ajoene and experiments using a single isomer had received little(More)
Recent data have shown that [125I]D-Ala2, MePhe4, Met(o)ol5-enkephalin (FK-33-824) is a highly selective and specific mu opioid receptor ligand [Moyse et al. (1986) Peptides 7, 351-355]. This probe was used here to investigate the detailed radioautographic distribution of mu sites at various levels of the spinal cord. [125I]FK-33-824 binding sites were(More)
In naive mice, ibogaine at a tremorigenic dose (30 mg/kg, ip), did not produce antinociception but did potentiate the antinociceptive potency of morphine in the tail-flick test. In morphine-dependent mice, ibogaine did not eliminate withdrawal symptoms but significantly increased the number of repetitive vertical jumps induced by naloxone, whatever the(More)
The autoradiographic distribution of mu, delta and kappa opioid binding sites was evaluated in various segments of the rat and guinea pig spinal cord. Mu opioid receptor binding sites are highly concentrated in the superficial layers of the dorsal horn (laminae II and III) in both species, without any marked gradient along the cord. Delta binding sites are(More)
Dynorphin A, which displays a wide variety of physiological effects, binds to opioid receptors preferentially at the kappa receptor type. kappa-selective antagonists would be very useful as pharmacological and biochemical probes to study and better understand the action of dynorphin A at its preferred receptor. However, the development of such molecules has(More)
The objectives of this study were to compare the pharmacokinetic properties and the duration of analgesia following intrathecal administration (L5-S1) of 2 mg morphine in 2 forms: (1) an isobaric (NaCl 0.9%) and (2) a hyperbaric solution (7% dextrose). The study was carried out on 5 cancer patients with severe, intractable pain in the lower half of the(More)
1. In the search for kappa-opioid antagonists, we have designed two N,N-diallyl substituted analogues of the kappa-selective peptide [D-Pro10]dynorphin A (1-11)(DPDYN). In this study, we have examined (i) the binding properties of N,N-diallyl-DPDYN (analogue 1) and N,N-diallyl-[Aib2,3]DPDYN (analogue 2) at the three main types (mu, delta, kappa) of opioid(More)
1 Development of the analgesic response to morphine and ontogenesis of central opiate receptors were analyzed in rats 5 to 120 days old. 2 The analgesic effect of morphine increased until day 15, after which it decreased to reach a plateau at about day 30. With phenoperidine, on the other hand, the analgesic effect increased until day 15, remained constant(More)
The mono- and diiodinated derivatives of the kappa-selective ligand [D-Pro10]dynorphin(1-11), DPDYN, were prepared. Their binding properties at the three opioid receptor types (mu, delta and kappa) were examined and compared to those of the parent peptide. The monoiodo derivative shows a general although moderate decrease in affinity and retains high kappa(More)