Changes in LHRH in human maternal plasma during pregnancy.
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Chorionic Gonadotropin↗
Biomedical subjects
K Tasaka
Publications and source records attributed to K Tasaka.
Effects of H1-receptor blocking drugs on the frog sartorius neuromuscular junction.
The effects of H1-receptor blocking agents, pyrilamine, promethazine, and diphenhydramine, on the amplitude and time course of endplate potentials (e.p.ps) were studied in the sartorius muscles of frogs. H1-receptor blockers (10(-5)-10(-4) M) reduced the amplitude of e.p.ps recorded intracellularly without affecting the resting membrane potential. The acetylcholine potential was decreased by perfusion of H1-receptor blockers. However, when the muscle fibre was stimulated directly, threshold and magnitude of action potential were not affected by H1-receptor blockers. The time constant of decay of the e.p.ps recorded extracellularly was reduced by H1-receptor blockers and the decay remained exponential with a single time constant. The quantal content was not reduced by perfusion of H1-receptor blockers at a concentration of 10(-4) M. It is assumed that the major site of action of these H1-receptor blocking agents is at the postsynaptic membrane.
Action Potentials↗
Hyaluronidase-inhibitory and anti-allergic activities of the photo-irradiated products of tranilast.
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Animals↗
Suppressive effect of prolactin on oestrogen-induced secretion of LH by sequentially perifused rat hypothalamus-pituitary.
The effect of prolactin (Prl) on oestrogen-induced gonadotrophin secretion was examined in vitro in a sequential double chamber perfusion system. As control groups, mediobasal hypothalamus (MBH)-pituitary pairs or pituitaries without the MBHs were perifused with Medium 199. As an experimental group, MBH-pituitary pairs were perifused with Medium 199 containing 1 micrograms/ml of rat Prl. These groups were stimulated with 10(-7) M oestradiol-17 beta (E2) for 30 min, and luteinizing hormone (LH) in the serial fractions of effluent was measured. In the control group of MBH-pituitary pairs perifused with medium without Prl, secretion of LH began to rise within 30 min after the beginning of stimulation, reached a peak 30 min after the end of stimulation and then remained at a plateau for the rest of the experimental period, whereas in the control group of pituitaries alone no significant response was observed. In the experimental group perifused with medium containing Prl, LH-secretion showed peaks 20 and 80 min after the end of E2-stimulation, respectively, and the first peak was significantly (P less than 0.01) less than the level in the control group. These data demonstrate that Prl at this concentration suppressed the rapid LH release induced by E2. Its site of action is suggested to be at the hypothalamic level, and its possible mechanism of action is discussed.
Animals↗
Epidermal growth factor stimulates secretion of rat pituitary luteinizing hormone in vitro.
The effects of epidermal growth factor (EGF) on pituitary luteinizing hormone (LH) release and on the releases induced by oestradiol (E2) and LH-releasing hormone (LRH) were examined in a sequential double chamber perifusion system. In this system the mediobasal hypothalami (MBH) and/or pituitaries excised from normally cycling female rats in dioestrus were perifused with test media. Perifusion with EGF at 1 ng/ml for 30 min induced significant release (80-100% increase, P less than 0.05) of LH from hypothalamo-pituitary pairs, but not from the pituitary alone. Perifusion of the pituitary alone with medium containing 1 ng/ml EGF, resulted in significant release of LH (70-140% increase, P less than 0.05) after administration of 10(-7) M E2, but did not significantly influence LH release in response to 20 ng/ml LRH. These findings suggest that EGF may be involved in the regulation of pituitary gonadotrophin secretion by a direct effect on the hypothalamus and indirectly by increasing the pituitary responsiveness to E2.
Animals↗
Possible site of negative and positive feedback action of oestrogen on gonadotrophin secretion in normal women.
For determination of the site of action of oestrogen (E) during the negative and positive feedback phases of gonadotrophin secretions, studies were made on the pituitary response to a small amount of LRH and the pulsatility of gonadotrophins after E administration in normal cycling women in the mid-follicular phase. The pituitary responses to an iv bolus of 2.5 micrograms of synthetic LRH were evaluated by measuring serum LH and FSH 2 h before and 8 h after administration of 20 mg of conjugated E (Premarin). In the next cycle, the pituitary responses to a same dose of LHRH were also observed 2 h before and 56 h after E injection. The mean levels of serum LH and FSH and the peak responses to LRH were significantly (P less than 0.05) decreased 8 h after E injection, but were significantly (P less than 0.05) increased 56 h after E administration. In the third cycle, the pulsatility of gonadotrophins was evaluated by measuring serum LH and FSH every 15 min for 180 min before and 8 h and 56 h after E injection. The pulse frequencies of gonadotrophins were not significantly different before and 8 h and 56 h after E injection. The amplitudes of pulses 56 h after Premarin injection were significantly higher than those before the injection. These findings suggest that the negative and positive feedback effects of E on gonadotrophin secretion may be caused, in part, by its direct action on the pituitary response to LRH.
Adult↗
Prolactin inhibits oestradiol-induced luteinizing hormone release at the pituitary level.
The direct action of prolactin (Prl) on pituitary LH secretion was studied by examining its effect on oestradiol (E2)-induced luteinizing hormone (LH) release from the rat pituitary in a perifusion system and determining the oestrogen receptor (ER) content of the pituitary in hyperprolactinaemic female rats. When the pituitary from rats in pro-oestrus was perifused with medium alone, 10(-7) M E2 significantly (P less than 0.05) increased the LH concentration in the effluent by 60-130% of the basal level, but in medium containing 1 microgram/ml Prl it did not cause LH release. In hyperprolactinaemic rats produced by implanting 2 anterior pituitary glands under the kidney capsule, the ER content of the cytosol of the pituitary (53.2 +/- 2.9 fmol/pituitary) was significantly increased (P less than 0.05), but that of the nuclei (6.8 +/- 0.2 fmol/pituitary) was significantly decreased (P less than 0.05) compared with the contents in rats in pro-oestrus. These data suggest that Prl has a direct suppressive effect on LH secretion from the pituitary in the rat, and that decreased translocation of ER into the nucleus might relate to impaired LH release by E2 from the pituitary of hyperprolactinaemic rats.
Animals↗
Decrease of LRH receptors in the pituitary gland in streptozotocin-induced diabetic rats.
In studies into the mechanism of anovulation in the diabetic condition, the LRH receptor content of the pituitary gland of rats with diabetes mellitus was determined. Normal female rats weighing 180-200 g were injected iv with either streptozotocin (6 mg/100 g body weight) or vehicle in dioestrus of the oestrous cycle. The rats were sacrificed by decapitation 9 days after treatment, and serum LH concentrations and the LRH content of the medial basal hypothalamus (MBH) were measured by radioimmunoassay (RIA), and the LRH receptor content of the pituitary gland was determined. The serum concentration of LH and the LRH content of the MBH in diabetic rats were 34.4 +/- 4.8 ng/ml (mean +/- SEM) and 2.05 +/- 0.04 ng/MBH, respectively, which were similar to the respective values of normal rats in dioestrus. However, the LRH receptor content of diabetic rats (13.2 +/- 3.9 fmol/pituitary) was significantly (P less than 0.05) lower than that of normal rats in dioestrus (68.0 +/- 7.1 fmol/pituitary) and pro-oestrus (59.4 +/- 13.6 fmol/pituitary). These results suggest that anovulation in diabetic rats is at least partly attributable to a low content of LRH receptors in the pituitary gland.
Animals↗
Hypotensive effects of dihydropyridine derivatives.
Effects of six dihydropyridine derivatives (nifedipine, nisoldipine, nitrendipine, nicardipine, nimodipine and niludipine) and hydralazine on blood pressure and heart rate in spontaneously hypertensive rats (SHR) were studied in comparison with those in normotensive rats (NR). Nisoldipine, nitrendipine and nicardipine showed stronger hypotensive effect in SHR than in NR. All the dihydropyridine derivatives--especially nifedipine, nitrendipine and niludipine--lowered blood pressure of SHR at doses smaller than those producing positive chronotropic effect. Hydralazine caused hypotensive effect in the same extent both in SHR and in NR and, moreover, it brought about tachycardia at doses smaller than those lowering blood pressure.
Animals↗
[Stimulatory effect of a traditional herbal medicine, Unkeito on LH-RH release].
In order to study the effect of Unkeito (Chinese name, Wen-Jan-Tang), a traditional Chinese herbal medicine and its components on luteinizing hormone-releasing hormone (LH-RH) and LH release, the mediobasal hypothalamus (MBH) alone or the pituitary alone or the pituitary in sequence with the MBH from normal female rats in diestrus was perifused in a sequential double-chamber perifusion system. LH-RH release from MBH increased significantly (p less than 0.05) by 50-100% of the basal level 30-90 min after the beginning of Unkeito administration. Unkeito at 5 micrograms/ml induced significant LH release (60-95% increase) from the pituitary in series with the MBH, but had no effect on LH release from the pituitary perifused alone. One of Unkeito's components Botanpi induced significant LH release, although other five components had no effect on LH release. These data suggest that Unkeito induces LH release from the pituitary through hypothalamic LH-RH, and can be used for the treatment of patients with hypothalamic amenorrhea.
Animals↗
Permeability increase in black lipid membrane induced by compound 48/80.
When compound 48/80, a potent histamine liberator, was added in the aqueous phase facing the black lipid membrane, the conductivity of the membrane was remarkably increased. Although valinomycin displayed a distinct selectivity for K+ movement, such selection for ionic permeability was not observed in the case of compound 48/80.
Animals↗
Effect of pituitary transplants on the LH-RH concentrations in the medial basal hypothalamus and hypophyseal portal blood.
The effects of hyperprolactinemia on catecholamine turnover in the medial basal hypothalamus (MBH) and on the luteinizing hormone-releasing hormone (LH-RH) concentrations in MBH and hypophyseal portal blood were investigated in female Wistar rats. Chronic endogenous hyperprolactinemia was produced by implantation of anterior pituitary glands under the kidney capsule. Catecholamine turnover in the MBH was studied by inhibiting monoamine oxidase and then measuring the accumulation of catecholamines by high-performance liquid chromatography with electrochemical detection. Rats bearing pituitary transplants exhibited: (1) persistent vaginal diestrus within 3-6 days of the implantation; (2) increased serum concentrations of prolactin (PRL); (3) decreased serum concentrations of luteinizing hormone (LH); (4) increased pituitary concentrations of LH and follicle-stimulating hormone (FSH); (5) increased turnovers of dopamine in the MBH; and (6) decreased concentrations of LH-RH in the MBH and in plasma of hypophyseal portal blood. These findings suggest that chronic hyperprolactinemia may increase dopaminergic tone in the MBH that may inhibit LH-RH secretion from the MBH, and LH release from the pituitary. These processes may be responsible for disturbances of cyclic pituitary-ovarian activity.
Animals↗
Effect of N-methylation of phosphatidylethanolamine on the fluidity of phospholipid bilayers.
The effect of N-methylphosphatidylethanolamine on phase transition and the fluidity of the liposomes made of dipalmitoylphosphatidylcholine or phosphatidylethanolamine was studied by the steady-state fluorescence polarization method and differential scanning calorimetry. N-methylation of phosphatidylethanolamine caused a decrease of fluidity of liposomes made of dipalmitoylphosphatidylcholine, but had little effect on dipalmitoylphosphatidylethanolamine. The liposomes prepared with both phosphatidylcholine and N-methylphosphatidylethanolamine and also phosphatidylethanolamine and N-methylphosphatidylethanolamine could be composed of solid solution and exhibited symmetric phase diagram.
Animals↗
Analgesic effect of histamine induced by intracerebral injection into mice.
Three methods were used to study the analgesic effect of intracerebral injection of histamine (Hi) on mice: the writhing test (acetic acid and phenylquinone), the electrical stimulation of the tail and the hot plate test. At doses higher than 2 micrograms, Hi inhibited the writhing syndrome significantly, and at doses of 10 micrograms or higher, Hi displayed a marked analgesic effect during both the electrical stimulation and hot plate methods. The saline injection produced only a negligible effect. Simultaneous application of Hi and 10 micrograms of diphenhydramine, pyrilamine or promethazine, apparently causing no analgesic effect from a single administration, caused a parallel shift of the dose-response curve of Hi to the right. ED50 of Hi was increased approximately 2, 2.8 and 3.8 times, respectively. However, cimetidine did not reveal any antagonistic effect on Hi-induced analgesia. Subcutaneously administered, 3 mg/kg of morphine augmented the analgesic effect of Hi. In accordance with this, pretreatment of naloxone (0.005 mg/kg) antagonized the analgesic action of Hi almost completely. When 5 mg/kg of leucine-enkephalin, less than the minimum effective dose, was given prior to Hi injection, the analgesic effect of Hi was enhanced. In addition, 10 and 20 micrograms of Hi increased the morphine analgesia markedly and parallel shifted the dose-response curve of morphine to the left.
Analgesics↗
Effect of histamine on the hippocampal neurons in guinea-pigs.
Histamine produced an excitatory effect on CA3 pyramidal cells in hippocampal slices of guinea-pigs. The amplitude of population spikes and EPSPs was augmented by histamine at concentrations of 10(-7) to 10(-6) M. Cimetidine but not pyrilamine prevented the stimulatory effect. The histamine effect was mimicked by dimaprit but not by 2-pyridylethylamine. It is concluded that histamine has a facilitatory influence on the hippocampal excitatory system via H2 receptor.
Animals↗
High immune complex level in healthy middle aged females.
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Adolescent↗
Epileptogenic activity induced by intravenous injection of certain cephalosporins in rats.
Epileptogenic activity induced by intravenous injection of certain cephalosporin derivatives was studied. Ceftezole provided the most potent epileptogenic activity among the drugs tested. Changes in seizure patterns on electroencephalogram (EEG) tracings and behavioral signs after administration of cefotiam and cefazolin were similar to those seen after ceftezole, though the intensity and duration were less than those of ceftezole. Cephacetrile and cephaloridine elicited the spiking activity in the frontal cortex and the other regions without apparent behavioral changes. Latamoxef and cefmenoxime displayed a weak epileptogenic activity at a dose of 1000 mg/kg. On the other hand, cephapirin, cefmetazole and cefoxitin did not evoke any changes in EEG nor in behavior. Penicillin G at a dose of 200 mg/kg affected spike or spike-and-wave complex in a few cases, but at a dose of 500 mg/kg the animals died of dyspnea almost immediately after injection without showing apparent epileptogenic signs. These results suggest that some of cephalosporins such as ceftezole, cefotiam, cephacetrile and cefazolin provide epileptogenic activity at higher doses.
Animals↗
Synthesis and structure-activity relationship of spiro[isochroman-piperidine] analogs for inhibition of histamine release. IV.
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Animals↗