Assessment of the adrenergic effects of orphenadrine in rat vas deferens.

Article Details

Citation

Pubill D, Canudas AM, Pallas M, Sureda FX, Escubedo E, Camins A, Camarasa J

Assessment of the adrenergic effects of orphenadrine in rat vas deferens.

J Pharm Pharmacol. 1999 Mar;51(3):307-12.

PubMed ID
10344632 [ View in PubMed
]
Abstract

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. In the low micromolar range, orphenadrine enhanced electrically-evoked and exogenous noradrenaline contractile responses in the epididymal portion of rat vas deferens. It also induced spontaneous activity that was inhibited by prazosin (1 microM) but not by atropine (20 nM). It inhibited accumulation of [3H]noradrenaline in rat vas deferens (IC50 = 14.2+/-2.3 microM). Orphenadrine competitively inhibited [3H]nisoxetine binding in rat vas deferens membranes (Ki = 1.05+/-0.20 microM). It can be concluded that orphenadrine, at low micromolar concentrations, interacts with the noradrenaline reuptake system inhibiting its functionality and thus potentiating the effect of noradrenaline.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
OrphenadrineSodium channel protein type 10 subunit alphaProteinHumans
Unknown
Inhibitor
Details
OrphenadrineSodium-dependent noradrenaline transporterProteinHumans
Yes
Inhibitor
Details