Effects of vinconate on neurotransmitter receptor systems in aged rat brain

We investigated the effects of age and (±)-methyl-3-ethyl-2,3,3a,4-tetrahydro-1 H-indolo[3,2,1-de][1,5]naphthyridine-6-carboxylate hydrochloride (vinconate), an indolonaphthyridine derivative, on neurotransmitter receptor systems in the rat brain using quantitative receptor autoradiography. [(3)H]Quinuclidinyl benzilate (QNB), [(3)H]hemicholinium-3 (HC) and [(3)H]muscimol were used to label acetylcholine receptors, high-affinity choline uptake sites and γ-aminobutyric acid(A) (GABA(A)) receptors, respectively. [(3)H]QNB, [(3)H]HC and [(3)H]muscimol binding decreased in any brain areas of 24-month-old (aged) rats in comparison with 6-month-old (adult) Animals. Chronic treatment with vinconate (10 and 30 mg/kg, i.p., once a day for 4 weeks) partly ameliorated the reduction in [(3)H]QNB, [(3)H]HC and [(3)H]muscimol biding in aged rat brains. This effect was especially noted in [(3)H]muscimol binding. The results suggest that vinconate may have beneficial effects on age-related changes in neurotransmitter receptor systems.