Effects of vinconate on specifically impaired short-term memory were studied in rhesus monkeys. Monkeys were trained to perform for orange juice reinforcement under a matching-to-sample response procedure. In the procedure, monkeys had to choose one of two stimuli that had the same color as the sample stimulus. Half of a daily session consisted of simultaneous trials where the sample stimulus was present during the time of choice. The other half of the session consisted of delayed trials where the sample stimulus had been presented but withheld at the time of choice. After the repeated training, the matching-to-sample responses were established with the percentage of correct choice responses (CR%) in both types of trials exceeding 90%. The doses of scopolamine, intervals between administration of this drug and the start of test session, and delay times in delayed trials were adjusted from one monkey to another so that delayed matching-to-sample responses were impaired by scopolamine while simultaneous matching-to-sample responses were less impaired by this drug. Scopolamine (32 or 45 micrograms/kg, s.c.) decreased the CR% for delayed trials more markedly than the CR% for simultaneous trials in four monkeys. Intragastrically administered vinconate at 16 mg/kg attenuated the scopolamine-induced short-term memory impairment. These results suggested that vinconate possesses specific ameliorating action on memory impairment caused by hypofunction of the cholinergic system in the brain.

01 Apr 1997·Mechanisms of Ageing and DevelopmentQ2 · MEDICINE

Effects of vinconate on age-related alterations in [3H]MK-801, [3H]glycine, sodium-dependent d-[3H]aspartate, [3H]FK-506 and [3H]PN200-110 binding in rats

Q2 · MEDICINE

Article

Author: Fujiwara, Takehiko ; Kato, Hiroyuki ; Nagaki, Sumiko ; Shuto, Katsuro ; Itoyama, Yasuto ; Araki, Tsutomu

We investigated the effects of age and (+/-)-methyl-3-ethyl-2,3,3a,4-tetrahydro-1 H-in-dolo[3,2,1-de] [1,5] naphthyridine-6-carboxylate hydrochloride (vinconate), an indolonaphthyridine derivative, on calcium channels, neurotransmitter receptor systems and immunophilin in Fischer rat brain using quantitative receptor autoradiography. [3H]MK-801, [3H]glycine, sodium-dependent D-[3H]aspartate, [3H]FK-506 and [3H]PN200-110 were used to label N-methyl-D-aspartate (NMDA) receptors, glycine receptors, excitatory amino acid transport sites, FK-506 binding proteins (FKBP) and voltage-dependent L-type calcium channels, respectively. [3H]Glycine and sodium-dependent D-[3H]aspartate binding significantly decreased in the frontal cortex, parietal cortex, striatum, nucleus accumbens, hippocampus, thalamus, substantia nigra and cerebellum of 24 month old rats in comparison with 6 month old animals. In contrast, [3H]MK-801, [3H]FK-506 and [3H]PN200-110 binding showed no significant changes in the brain of 24 month old rats. Intraperitoneal chronic treatment with vinconate (10 and 30 mg/kg, once a day for 4 weeks) dose-dependently ameliorated the significant reduction in [3H]glycine and sodium-dependent D-[3H]aspartate binding in the brain of 24 month old rats. These results demonstrate that glycine receptors and excitatory amino acid transport sites are more susceptible to aging processes than NMDA receptors, immunophilin and voltage-dependent L-type calcium channels. Furthermore, our findings suggest that vinconate may have a beneficial effect on age-related changes in glycine receptors and excitatory amino acid transport sites.

01 Feb 1997·Behavioural Brain ResearchQ3 · PSYCHOLOGY

Vinconate, a cognitive enhancer, and PI turnover-phospholipase C systems in the brain

Q3 · PSYCHOLOGY

Article

Author: Masashi Katsura ; Jun Xu ; Seitaro Ohkuma ; Toshiaki Iino ; Kinya Kuriyama

The molecular mechanisms for the stimulation of inositol 1-phosphate (IP1) formation by vinconate were investigated using preparations of rat brain. Vinconate (10(-8)-10(-3) M) dose-dependently inhibited the binding of [3H]quinuclidinyl benzilate ([3H]QNB) to muscarinic acetylcholine receptors and its IC50 value for [3H]QNB binding was 1.7 x 10(-5) M. The rightward shift of carbachol displacement curve of [3H]QNB binding by GTP (10(-4) M) was completely abolished by vinconate (10(-5) M). Carbachol (10(-8)-10(-2) M) increased [3H]IP1 formation in a dose-dependent manner and the carbachol-induced [3H]IP1 formation was significantly accentuated by vinconate (10(-5) M). The enhancement of [3H]IP1 accumulation by vinconate was inhibited by approximately 50% in the presence of atropine (10(-5) M), although phentolamine and ketanserin had no effects on the stimulatory effect of vinconate on [3H]IP1 formation. Vinconate showed no alteration in the binding of [3H]guanosine 5'-(beta, gamma-imino) triphosphate ([3H]Gpp(NH)p) to the crude synaptic membranes. The enhancement of phosphatidylinositol 4,5-biphosphate (PIP2)-specific phospholipase C (PLC) activity by GTP was unaffected in the presence of 10(-3) M vinconate, whereas vinconate alone dose-dependently enhanced the activities of both PIP2-specific and cytosolic PLC. These results suggest that vinconate may induce the facilitation of phosphatidylinositide (PI) turnover via the stimulation of muscarinic acetylcholine receptors, the enhancement of coupling between muscarinic acetylcholine receptors and GTP-binding protein, and the direct activations of PIP2-specific and cytosolic PLC.

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Indication	Highest Phase	Country/Location	Organization	Date
Cognition Disorders	NDA/BLA	-	Ajinomoto Co., Inc.	-
Cognition Disorders	NDA/BLA	JP	Mitsubishi Pharma Corp.	-
Cognition Disorders	NDA/BLA	-	Mitsubishi Tanabe Pharma Corp.	-
Stroke	NDA/BLA	-	Ajinomoto Co., Inc.	-
Stroke	NDA/BLA	-	Mitsubishi Tanabe Pharma Corp.	-

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