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anes.med.osaka-u.ac.jp
We tested the ability of electroconvulsive treatment (ECT) to block thermal hyperalgesia and mechanical allodynia in rats with peripheral neuropathy. Repeated ECT (six times daily) significantly reduced thermal hyperalgesia 48 h after the end of the final treatment but had no significant effects on mechanical allodynia. Single ECT had no significant effect on thermal hyperalgesia or mechanical allodynia. Neither single nor repeated ECT had any significant effect on the withdrawal response of sham-operated paws and untreated rats to thermal and mechanical stimuli. The anti-thermal hyperalgesic effect of repeated ECT was reversed by the previous administration of nifedipine (L-type Ca2+ channel blocker). We conclude that, due to effects on the voltage dependent calcium channel, ECT modified one of the pain behaviors induced by nerve injury. ECT may be of use in the treatment of human neuropathic pain. IMPLICATIONS: We showed that repeated electroconvulsive treatment reduced pain responses to heat stimulation after sciatic nerve injury in rats. This study implies a possible therapeutic effect of electroconvulsive treatment on neuropathic pain.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9495420&dopt=Abstract
Psychopharmacology (Berl). 1990;101(2):240-3.
Effect of repetitive electroconvulsive treatment on sensitivity to pain and on [3H]nitrendipine binding sites in cortical and hippocampal membranes.
Antkiewicz-Michaluk L, Michaluk J, Romanska I, Vetulani J.
Department of Biochemistry, Polish Academy of Sciences, Krakow, Poland.
The effect of electroconvulsive shock (ECS) on the responsiveness to pain (measured by the hot-plate test) and on the characteristics of L-type calcium channels (measured as [3H]nitrendipine binding sites) in the cortex and hippocampus was tested on the Wistar rat. In animals receiving a single ECS, the calcium channel density and affinity 24 h after treatment did not differ from the controls; the response to pain was also at the control level. Repeated ECS (eight once-daily shocks) resulted in an increased responsiveness to pain (shortening of response latency) and in an increase in the density of cortical, but not hippocampal, calcium channels. The KD value for [3H]nitrendipine binding sites in either brain region remained unaltered by ECS. The calcium channel antagonist nifedipine, which by itself did not significantly alter the response to pain, prevented the enhancement of pain sensitivity brought about by ECS. The results suggest activation of calcium-dependent mechanisms by repeated ECS and confirm the involvement of calcium channels in pain mechanisms.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2161550&dopt=Abstract
Arzneimittelforschung. 1993 Jul;43(7):722-8.
In vitro and in vivo electrocardiographic evaluation of the novel calcium antagonist monatepil on cardiac conduction system.
Nose I, Kataoka T, Honda Y, Yamada T, Ikeno A, Fukuya F, Minato H, Takeyama K, Hosoki K, Karasawa T.
Department of Pharmacology, Dainippon Pharmaceutical Co., Ltd., Suita, Osaka, Japan.
Effects of monatepil ([(+/-)-N-(6,11-dihydrodibenzo[b, e]thiepin-11-yl)-4-(p-fluorophenyl)-1-piperazinebutyramide]m aleate, AJ-2615, CAS 103377-41-9), a novel calcium antagonist, on the cardiac conduction system were compared by electrocardiography with those of the existing calcium antagonists (diltiazem, verapamil and nifedipine) in isolated rabbit heart preparations in vitro and in anesthetized and conscious dogs in vivo. Monatepil (10(-7) mol/l) prolonged the atrio-His bundle conduction time (AH interval) in the Langendorff perfused rabbit heart, like diltiazem, verapamil and nifedipine. This prolongation was decreased to 1/10 in the presence of 3.6% bovine serum albumin. In anesthetized dogs, monatepil (0.1-1.0 mg/kg i.v.), unlike diltiazem and verapamil, did not prolong AH interval. In conscious dogs, monatepil even at 100 mg/kg p.o. did not affect electrocardiograms. At the high dose of 300 mg/kg p.o., only a slight prolongation of the QT interval was found, but the QTc interval was not affected. Diltiazem at 10 mg/kg p.o. caused a prolongation of the PR interval and a disappearance of QRS waves. In conscious renal hypertensive dogs, repeated administration of monatepil (10 mg/kg/d p.o. for 29 days) had little effect on the conduction system of the heart examined by electrocardiograms, albeit a persistent fall in blood pressure continued throughout the administration period. The above results suggest that monatepil is a highly safe drug in the treatment of hypertension.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8369002&dopt=Abstract
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