Assessment of the Adrenergic Effects of Orphenadrine in Rat Vas Deferens

  title={Assessment of the Adrenergic Effects of Orphenadrine in Rat Vas Deferens},
  author={David Pubill and A. M. Canudas and Merc{\'e} Pall{\`a}s and Francesc X Sureda and Elena Escubedo and Antoni Camins and Jorge Camarasa},
  journal={Journal of Pharmacy and Pharmacology},
The peripheral adrenergic effects of orphenadrine, an antiparkinsonian drug, have been evaluated in the rat vas deferens to investigate whether these properties are the same as those of other phencyclidine ligands. 
Orphenadrine-induced convulsive status epilepticus in rats responds to the NMDA antagonist dizocilpine.
Assessing the efficacy of a new generation antiepileptic drugs (AEDs) and some of the experimental agents in suppressing ORPH-evoked seizures in rats suggested that NMDA activation is partly involved in the proconvulsant activity of orphenadrine but may not be the primary pathomechanism.
Involvement of voltage-gated sodium channels blockade in the analgesic effects of orphenadrine
Orphenadrine affinities for resting and inactivated sodium channels were higher compared to those of known sodium channels blockers, such as mexiletine and flecainide, indicating a role for sodium channel blockade in the clinical efficacy of or phenadrine as analgesic compound.
Comparison of the Analgesic Effects of a Fixed-Dose Combination of Orphenadrine and Diclofenac (Neodolpasse®) with its Single Active Ingredients Diclofenac and Orphenadrine
The observed effect was mainly caused by central mechanisms and was found to be superior for the fixed-dose combination of orphenadrine and diclofenac compared with the individual ingredients, which can be explained by the different molecular mechanisms of action of each drug.
[New treatment options for piriformis syndrome].
Modern approaches to the diagnosis and management of patients with piriformis syndrome are discussed, and new possibilities of treating this syndrome using a fixed combination of diclofenac and orphenadrine registered in the Russian Federation as a drug for intravenous infusion neodolpasse are discussed.
Pain: Physiologic background and therapeutic Consequences
A better understanding of the mechanisms involved in perception and transmission of nociceptive inputs as well as peripheral and central downregulating feedback may help to create individualize analgesic treatment regimens for complicated pain syndromes.


Glutamate and kainate effects on the noradrenergic neurons innervating the rat vas deferens
It is concluded that noradrenergic neurons of the vas deferens are under glutamatergic control and that this might be important in the motor control of the organ.
Inhibition of orphenadrine of 3H-dl-noradrenaline and 14C-tyramine uptake in atria.
Abstract Orphenadrine reduced the accumulation of radioactivity by guinea pig atria incubated with either 3 H- dl -noradrenaline or 14 C-tyramine, indicating an inhibition of the uptake of these
MK-801 enhances noradrenergic neurotransmission in rat vas deferens.
Since these effects took place in the presence of magnesium and were sodium-dependent, a direct participation of the NMDA receptor complex can be ruled out, pointing to the inhibition of the cathecolamine uptake systems in the postganglionic sympathetic nerve endings as the most feasible mechanism.
Characterization of [3H]nisoxetine binding in rat vas deferens membranes: modulation by sigma and PCP ligands.
Results suggest that sigma and PCP ligands bind, at low micromolar concentrations, to a site in the noradrenaline transporter that is labelled by [3H]NIS.
Comparison of amantadine, orphenadrine, and placebo in the control of phenothiazine-induced Parkinsonism.
The findings of the present study are not conclusive but show a clear need for further research in this field and the paucity of evidence for the effectiveness of anti-cholinergic drugs in both Parkinson's disease and in drug-induced Parkinsonism.
Influence of orphenadrine HCl and its N-demethylated derivatives on the in vitro uptake of noradrenaline and 5-hydroxytryptamine by rat brain slices
Abstract Among a number of compounds tested for their influence on the uptake of radioactive noradrenaline (NA) and 5-hydroxytryptamine (5-HT) by rat brain slices, imipramine appeared to be the
Are NMDA antagonistic properties relevant for antiparkinsonianlike activity in rats?—Case of amantadine and memantine
It can be assumed that the doses of amantadine, memantine and MK-801 showing antiparkinsonian-like activity in animals result in plasma levels leading to NMDA antagonism, but in the haloperidol-induced catalepsy test the efficacy of amanadine was higher than memantine, while the opposite was true for rotation and reserpine-induced sedation indicating pharmacodynamic differences between both agents.
l-Glutamic acid, a neuromodulator of dopaminergic transmission in the rat corpus striatum
It is suggested that during depolarization a Ca(2+)-dependent event occurs at the striatal membrane level which changes the sensitivity of the dopamine release process to neuroexcitatory aminoacids in such a way as to render it relatively more specific and stereoselective towards l-glutamate stimulation.
Role of the sigma receptor in the inhibition of [3H]-noradrenaline uptake in brain synaptosomes and adrenal chromaffin cells.
The results indicate that the central and peripheral inhibitory effects of PCP and sigma-receptor ligands on [ 3H]-NA uptake involves a receptor (sigma 1-like) which is distinct from that (PCP2) recognized for the inhibition of [3H]-dopamine uptake by PCP.
Role of the σ receptor in the inhibition of [3H]‐noradrenaline uptake in brain synaptosomes and adrenal chromaffin cells
1 Rat brain synaptosomes and cultured bovine adrenal chromaffin cells were used to monitor the inhibitory effects of phencyclidine (PCP) and sigma (σ)‐receptor ligands on the uptake of