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Dynorphin A (dynA) and related opioid peptides produce moderate analgesic effects with restricted types of pain stimuli that are often accompanied by a large variety of naloxone-insensitive biochemical and behavioural effects. In binding assays in vitro, dynA possesses a high affinity for mu-, delta- and kappa- opioid receptors with some selectivity for(More)
The antinociceptive effects of intracerebroventricular (ICV) administration of histogranin (HN) and related peptides were assessed in the mouse writhing and tail-flick assays. In the writhing test, the peptides displayed dose-dependent analgesic effects with an AD(50) of 23.9 nmol/mouse for HN and the following order for other peptides: HN-(7-15)<histone(More)
1. Rat brain synaptosomes and cultured bovine adrenal chromaffin cells were used to monitor the inhibitory effects of phencyclidine (PCP) and sigma (sigma)-receptor ligands on the uptake of [3H]-noradrenaline ([3H]-NA). 2. A Na(+)-dependent high affinity uptake was observed in synaptosomes (30 degrees C) and chromaffin cells (37 degrees C) with Km of 0.22(More)
Dynorphin A-(1-13) and related peptide fragments were tested for their ability to modulate the binding of the competitive NMDA receptor antagonist, [3H]2-amino-4-propyl-5-phosphono-3-pentanoic acid ([3H]CGP-39653), to rat brain membranes. Dynorphin A-(1-13) produced a dose-dependent (1 nM to 10 microM) potentiation of [3H]CGP-39653 binding. The potentiation(More)
Dynorphin A-(1-13)-Tyr-Leu-Phe-Asn-Gly-Pro (Dyn Ia; 1-8 nmol) injected intracerebroventricularly in the mouse produces two independent behavioral effects: (1) a norbinaltorphimine (kappa opioid antagonist)-reversible analgesia in the acetic acid-induced writhing test and (2) motor dysfunction characterized by wild running, pop-corn jumping, hindlimb jerking(More)
We develop an arbitrary-order primal method for diffusion problems on general polyhedral meshes. The degrees of freedom are scalar-valued polynomials of the same order at mesh elements and faces. The cornerstone of the method is a local (element-wise) discrete gradient reconstruction operator. The design of the method additionally hinges on a least-squares(More)
Dynorphin (Dyn) A and related opioid and nonopioid peptides were tested for their ability to produce motor effects in mice. Central (intracerebroventricular) administration of Dyn A in mice produced marked motor effects characterized by wild running, jumping, circling and/or barrel rolling with an ED50 value of 14.32 (95% confidence limits, 10.09-20.32)(More)
In this work we introduce a discrete functional space on general polygonal or polyhedral meshes which mimics two important properties of the standard Crouzeix–Raviart space, namely the continuity of mean values at interfaces and the existence of an interpolator which preserves the mean value of the gradient inside each element. The construction borrows(More)
The effect of dynorphin A (Dyn A)-related peptides and nociceptin on the binding of the D2 receptor antagonist, [(3)H]raclopride, was examined in membrane preparations of rat heart. Non-linear regression saturation binding analysis of [(3)H]raclopride binding revealed the presence of a single high-affinity binding site with a K(d)of 4.1 n M and a B(max)of(More)
The behavioral and pharmacologic profiles of [Ser1]histogranin ([Ser1]HN) were assessed by monitoring its ability to displace the binding of the specific N-methyl-D-aspartate (NMDA) receptor ligand, [3H]CGP 39653, to block the convulsant effects of NMDA and other excitatory agents in mice, and to produce phencyclidine (PCP)-like behavioral effects in rats.(More)