Drugs online research references
Can J Physiol Pharmacol. 1990 Aug;68(8):1093-9.
Effect of naloxone and prolonged preganglionic stimulation on noncholinergic transmission in the superior cervical ganglion of the cat.
Bachoo M, Yip R, Polosa C.
Department of Physiology, McGill University, Montreal, Que., Canada.
In cats anesthetized with sodium pentobarbital, a supramaximal 40-Hz, 30-s train to the cervical sympathetic trunk, during block of ganglionic cholinergic transmission with hexamethonium and scopolamine, produced a delayed, slow, small amplitude contraction of the nictitating membrane that persisted for several minutes after the end of the stimulus train. The post-stimulus component of the response was due to afterdischarge of the ganglion cells, since section of the post-ganglionic axons at the end of the train resulted in elimination of this component. The amplitude of the slow nictitating membrane response was enhanced in a dose-dependent manner by i.v. injection of naloxone. The enhancement was detectable at a dose as low as 1 microgram/kg and was maximal at 10 micrograms/kg. During continuous preganglionic stimulation at 40 Hz, the amplitude of the slow nictitating membrane response reached a peak in 2-4 min and then faded with time until it became undetectable. Time for 90% decay was 82 +/- 5 min (n = 18). The nictitating membrane response to postganglionic nerve stimulation was not modified by prolonged preganglionic stimulation. In three cats, the cervical sympathetic trunk was split into two bundles and one bundle was stimulated continuously at 40 Hz until the slow response disappeared. At this time stimulation of the unconditioned bundle evoked a slow response of normal appearance. This suggests that the process underlying the fade involves only the conditioned axons. Recovery from the fade was slow, the response approaching control by 24 h post-stimulus.(ABSTRACT TRUNCATED AT 250 WORDS)
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2167765&dopt=Abstract
Nippon Yakurigaku Zasshi. 1987 Jun;89(6):323-9.
[Anti-amnesic effect of prolyl endopeptidase inhibitors in mice]
[Article in Japanese]
Nanri M, Kaneto H.
Based on the results of a previous report that prolyl endopeptidase (PPCE) inhibitors facilitated the acquisition of active avoidance response and retarded the extinction of the response, further studies were made on the effect of PPCE inhibitors on learning and the memory process. Using mice, tests were performed both in the light-dark discrimination Y-maze task and the lever-press task of the water reinforcement schedule, and mice were also tested in the acquisition and retention of one-trial "step-through" passive avoidance task. The effect of PPCE inhibitors were investigated both in control and electroconvulsive shock- or scopolamine-induced amnesic animals. Z-Pro-p, the most potent inhibitor among 5 compounds tested in this study, and arginine vasopressin (AVP) facilitated the learning process and retarded the extinction of the acquired response in all tests. Suc-Pro-p was also effective in the Y-maze and passive avoidance test. Thus, the effect of the test compounds were parallel with their in vitro activities as PPCE inhibitor. These results suggest that the anti-amnesic effect of PPCE inhibitors is partially attributable to their effect on the breakdown of the biologically active peptides which are involved in the memory process, such as AVP, in the brain.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3305244&dopt=Abstract
J Pharmacobiodyn. 1987 Dec;10(12):730-5.
Specific inhibitors for prolyl endopeptidase and their anti-amnesic effect.
Yoshimoto T, Kado K, Matsubara F, Koriyama N, Kaneto H, Tsura D.
Department of Biotechnology, School of Pharmaceutical Sciences, Nagasaki University, Japan.
Several peptides and peptide derivatives were tested for their inhibitory effect on prolyl endopeptidase and possible properties as anti-amnesic agents. Among the compounds tested, Z-Gly-Pro-CH2Cl, Z-Val-prolinal, Boc-Pro-prolinal, Z-Pro-prolinal, aniracetam and pramiracetam inhibited the enzyme activities at Ki values in the order of nM to microM, and the effect of the prolinal-containing peptide derivatives was specific for prolyl endopeptidase. Z-Pro-prolinal was the most effective inhibitor in vitro (Ki = 5 nM) and in vivo (50 to 70% inhibition in various organs of rat at a dose of 1 mumol/animal i.p.). Regional differences were observed in the effect of inhibitors on the brain enzyme activities: most active in mesencephalon, followed by striatum, cerebellum, hippocampus, hypothalamus; and inactive in cerebral cortex and medulla oblongata. In the passive avoidance learning test using rats, pretreatment with Z-Pro-prolinal prevented the induction of amnesia by scopolamine at the dose of 1 mumol/animal, i.p. Z-Val-prolinal, Z-Pyr-prolinal and Z-Gly-Pro-CH2Cl were also effective in the retention test at 24 and 48 h after the training trial. The antiamnesic effect of these compounds was approximately parallel to the in vitro inhibitory activities on prolyl endopeptidase. These results suggest the possibility that the inhibitors exhibit their anti-amnesic effect through the regulation of the enzyme activity in the brain.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3330562&dopt=Abstract
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