Haloperidol, a butyrophenone, was synthetized by Janssen and introduced for the treatment of psychosis. Although structurally different from the phenothiazines, the butyrophenones share many of their pharmacological properties, such as inhibition of conditioned avoidance response, blocking effect of amphetamine reaction, producing catalepsy, antishock effect and protection against the lethal effects of catecholalmines. Chlorpromazine can lower the arterial blood pressure through its adrenergic blocking activity, its direct effect in relaxing vascular smooth muscle, its direct effect in depressing the myocardium and its action in a complex manner on the central nervous system. In the case of haloperidol, however, was not clarified the mechanism of lowering the blood pressure. The present paper describes the effects of haloperidol on cardiovascular system to investigate the mechanisms of its actions on the arterial blood pressure. The results are followings; 1. In anesthetized cats, intravenous administration of haloperidol and chlorpromazine in the dose of 0.1mg/kg produced a slight decrease in the blood pressure, which followed by complete recovery within $30{\sim}60$ minutes. In the dose of 3mg/kg, however, both produced an abrupt and marked decrease of the blood pressure, which followed by delayed recovery. 2. Haloperidol in the dose ranges of 0.1mg to 3.0mg/kg tended to produce the heart rate slowing in the cats, while chlorpromazine has no effect on the rate. 3. Following administration of haloperidol or chlorpromazine, epinephrine reversal in the arterial blood pressure was observed in the cat, however the responses of norepinephrine and acetylcholine were little affected. 4. In the isolated rabbit atrium the contractility was depressed by haloperidol in the doses over 0.5mg per 100ml, but the rate was not affected. In contrast, the epinephrine-induced contractility was not depressed after haloperidol treatment. However, the increased rate of atrium by epinephrine was partially blocked after haloperidol. 5. In the isolated rabbit aortic strip, epinephrine-induced contraction was blocked by haloperidol. With the above results, it may be concluded that the hypotensive effect of haloperidol was largely due to ${\alpha}$-adrenergic blocking properties and the direct effect in depressing the myocardium as well as its action on central nervous system.
The purpose of this study was to investigate influence of wrist position on the electromyographic(EMG) activities of the flexor digitorum superficialis (FDS) and extensor digitorum (ED) during drilling and pinch grip. Eighteen healthy subjects had been recruited and each subject performed two tasks (drilling and pinch grip) at three different wrist positions ($30^{\circ}$ flexion, neutral, $30^{\circ}$ extension). The EMG amplitude of each muscle was normalized to the amplitude in the maximal voluntary contraction (MVC). Repeated one-way ANOVA was used to compare the differences of EMG across wrist positions. The FDS EMG activity in both drilling and pinch grip was lowest at $30^{\circ}$ wrist extension and the highest at $30^{\circ}$ wrist flexion. The ED EMG activity was lowest when the wrist was neutral in both tasks. From the results of this study, we can conclude that the desirable wrist positions for drilling and pinch grip tasks are slightly extended or neutral position. Therefore, flexed wrist position should be avoided to reduce the excessive work load on the finger muscles during the tasks.
Background: To prevent or reduce the risk of strain injury, various approaches, including stretching techniques are currently being used. The effect of proprioceptive neuromuscular facilitation (PNF) and static stretching on flexibility has been demonstrated; however, it is not clear which one is superior. Objects: This study aimed to evaluate the differences between the effects of PNF and static stretching performed at various intensities on muscle flexibility. Methods: The maximum voluntary isometric contraction (MVIC) of the hamstrings using the PNF stretching technique was performed in the P100 group, while 70% of the MVIC was performed in the P70 group. The MVIC value obtained during the PNF stretching in both groups was used as a reference for setting the intensity of static stretching. Static stretching was performed at 130% (S130), 100% (S100), and 70% of the MVIC (S70). The active knee extension (AKE) values, defined as the knee flexion angle were measured before stretching (baseline), immediately after stretching (post), and at 3 minutes, 6 minutes, and 15 minutes. Results: PNF stretching produce a greater improvement in flexibility compared with static stretching. Specifically, the ΔAKE was significantly higher in the S100 and S70 groups than in the P100 group at Post. In the comparison of ΔAKE over time in each group, the ΔAKE at Post showed a significant decrease compared to the value at Baseline in the S130 group; however, no significant difference was observed at 6 minutes while a significant increase was noted at 15 minutes. Conclusion: This study found that PNF stretching is more effective than static stretching with respect to increasing and maintaining the flexibility of muscles. In addition, the increase in flexibility at maximal intensity was similar to that observed at submaximal intensity during both PNF and static stretching.
To examine whether salt stress would alter or not contractility of isolated rat aorta, under anesthesia with sodium pentobarbital(50 mg kg-1 i.p.), male Sprague Dawley rats(300-330 g) were subjected to 0, 50, and 150 mM of sodium chloride at 37$^{\circ}C$ for 60 min. where as the sham group was left at modified Krebs-bicarbonate solution. To measure contractile response of vascular ring preparation isolated from rat was determined in organ bath and was recorded on physiograph connected to isometric transducer. And the strip was checked for expression of heat shock protein(Hsp) by Western blotting. One, three and eight hours later, we measured vascular contractility of isolated rat aorta treated with KCI, phenylephrine from organ bath study. The dose-vascular responses of potassium chloride and phenylephrine showed a little augmentation by NaCl concentration in the strips exposed to NaCl for 8 hours. And the response of relaxation induced by nitroprusside and acetylcholine was not influenced by NaCl stress in isolated aorta ring for 8 hours, respectively. Expression pattern of Hsp 70 of vascular muscle in isolated rat aorta showed a little increase in 150 mM NaCl group at 8 hours after NaCl treatment but not at 3 hours, and Hsp 60 expression of rat aorta was markedly increased in 50 mM NaCl group at 8 hours after NaCl treatment. Taken together, NaCl induced dose-and time dependent accumulation of the Hsp but not affected contraction of rat aorta. These data suggest that short term high salt stress was not sufficient to induce hypertension of rat aorta.
Tropomyosin (TM) is an important actin binding protein involved in regulation of muscle contraction. Unacetylated striated tropomyosin failed to bind to actin whereas unacetylated smooth tropomyosin bound well to actin. It has been demonstrated that high actin affinity of unacetylated ${\alpha}-tropomyosin$ was ascribed to the carboxyl terminal amino acid residues. In order to define the role of the carboxyl terminal residues of tropomyosin molecule on actin binding, two mutant tropomyosins were constructed. TM11 is identical to the striated tropomyosin except that the carboxyl terminal last three amino acids was replaced with $^{282}NNM^{284}$ whereas in TM14 $^{276}HA^{277}$ was substituted with smooth specific $^{276}QT^{277}$. TM11 and TM14 were overproduced in Escherichia coli and analyzed for actin affinity. The apparent binding constants (Kapp) of unacetylated tropomyosins were $2.2{\times}10^6M^{-1}$ for sm9, $1.03{\times}10^6M^{-1}$ for TM14, $0.19{\times}10^6M^{-1}$ for TM11, $>0.1{\times}10^6M^{-1}$ for striated, respectively. This result indicated that higher actin affinity of the unacetylated smooth tropomyosin was primarily attributed to the presence of QT residues in the smooth sequence. In case of the Ala-Ser (AS) dipeptide extension of the amino terminus of tropomyosin, Kapp were $21.1{\times}10^6M^{-1}$ for AS-sm9, $8.0{\times}10^6M^{-1}$ for AS-11, $4.7{\times}10^6M^{-1}$ for AS-14, $3.8{\times}10^6M^{-1}$ for AS-striated. AS-TM11 showed considerably higher actin affinity than AS-TM14, implying that interaction of Ala-Ser of the amino terminus with the carboxyl terminal residues. Since Kapp of AS-TM11 was significantly lower than that of AS-sm9, the presence of QT might be required for restoration of high actin affinity of the smooth ${\alpha}-tropomyosin$. These results suggested that the carboxyl terminal amino acid residues Glutamine275-Threonine276 are important for actin affinity of the recombinant smooth ${\alpha}-tropomyosin$, particularly of unacetylated smooth ${\alpha}-tropomyosin$.
The author confirmed the development of the smooth muscle in the oviduct proprius and anterior mesosalpinx in the leghorn, and observed that there was a variation between the action of norepinephrine on albumin-secreting portion of productive oviduct and that of non-productive one, and that $PGE_1$ might play a significant role on the activation of adrenergic ${\alpha}$-receptor in the non-productive oviduct. 1. There were many bundles of smooth muscles with irregular directions, which were identified in the both oviduct proprius and anterior mesosalpinx by Mallory aniline-blue orange G stain. 2. In vitro experiments, the anterior mesosalpinx was always relaxed by norepinephrine. While the albumin-secreting portion of non-productive period of oviduct was relaxed, but that of the productive one contracted by norepinephrine. Both the anterior mesosalpinx and oviduct proprius of chick responsed with relaxation to norepinephrine as shown in the non-productive hen. In vivo experiments, norepinephrine injected through the jugular vein increased the intraoviductal pressure in the productive oviduct, but decreased that in the non-productive one. 3. By treatment with $PGE_1$, in vitro, the relaxation induced not only by norepinephrine, but by periarterial electrical stimulation was converted into contraction, and in the presence of phentolamine, this conversion by $PGE_1$ was not shown. 4. The intra-oviductal pressure of the productive hen treated with indomethacin for 4 days was decreased by norepinephrine, but the increase in pressure by $PGE_1$ or $PGE_{2{\alpha}}$ was supersensitized when these drugs were administered through jugular vein. However, in vivo, the relaxation by norepinephrine was not converted into the stimulation after $PGE_1$ treatment. It might be summarized that the regulation of intra-oviductal pressure was dependent on the summation of the movement of both oviduct and mesosalpinx and intramurally produced prostaglandins contributes to the inherent tone of the prcductive oviduct by activating adrenergic ${\alpha}$-receptor.
Purpose: Menstruation is associated with menstrual symptoms like pain and balance problems which have an impact on the quality of life. Pilates increases pelvic stability and reduces menstrual pain by inducing abdominal muscle contraction. This study was done to evaluate the effects of Pilates on menstrual pain, symptoms, balance, and quality of life when compared to aerobic exercise. Methods: Thirty-nine women with menstrual pain were randomly divided into the Pilates group (n=13), aerobics group (n=13), and control group (n=13). The Pilates group performed lumbar-pelvic stabilization exercises, while the aerobic group ran on a treadmill. The control group did not undergo any intervention. The experimental groups exercised for four weeks (12 sessions) and did not exercise during menstruation. The Y-balance test was performed on the second day of menstruation to evaluate dynamic balance. The questionnaires administered immediately after menstruation were the visual analog scale (VAS), Korea Oswestry Disability Index (ODI), and the modified Menstrual Distress Questionnaire (MDQ). The paired t-test was used to compare the effect of exercise within the three groups and a oneway analysis of variance was used to compare between groups. Results: VAS and MEDI-Q scores significantly decreased in the Pilates group after 4 weeks compared with those in the aerobic and control groups. Moreover, ODI and Y-balance scores increased in the Pilates group compared with those in the aerobic and control groups (p<0.05). Conclusion: The Pilates stabilization exercises are effective and help in improving menstrual pain, balance and other menstrual symptoms assessed through ODI, and MEDI-Q, compared to aerobic exercises.
We have investigated the relative roles of α1-adrenoceptors and purinoceptors in contractions to low and high frequency stimulation of the mouse vas deferens, in terms of the time course of responses. In separate experiments, isometric contractile responses were obtained to 10 pulses at 1 Hz and 40 pulses at 10 Hz. Responses to 1 Hz stimulation consisted of a series of discrete peaks. The α1A-adrenoceptor antagonist RS100329 (10-9M-10-7M) significantly reduced the response to the first pulse, the α1D-adrenoceptor antagonist BMY7378 (10-7M-10-6M) significantly reduced the response to the first two pulses, and the non-selective α1-adrenoceptor antagonist prazosin (10-8M) reduced the response to the first 4 pulses at 1 Hz. Responses to 10 Hz stimulation consisted of an early peak response and a maintained plateau response. RS100329 significantly reduced the peak response but did not significantly affect the plateau response. Prazosin, significantly reduced both the peak and plateau responses. The α1A-adrenoceptor antagonist RS17053 in high concentrations reduced mainly the plateau response leaving a clear early peak response. The plateau response of contraction was almost abolished by the purinoceptor antagonist suramin. These results suggest that there is a relatively minor early α1D-adrenoceptor and a larger early α1A-adrenoceptor component to stimulationevoked contractions of mouse vas deferens, but the major α1-adrenoceptor component is revealed by prazosin to be α1B-adrenoceptor mediated. α1B-Adrenoceptor activation probably facilitates contractions mediated by other α1-adrenoceptors and by purinoceptors. These results suggest that combined non-selective α1-adrenoceptor blockade, particularly α1B-adrenoceptor blockade, in addition to P2X1-purinoceptor blockade is useful in reducing male fertility.
Shin, Han Jae;Gwak, Hyo Min;Lee, Moon Yong;Kyung, Jong Su;Jang, Kyoung Hwa;Han, Chang Kyun;Yang, Won Kyung;Kim, Seung Hyung
Korean Journal of Medicinal Crop Science
/
v.27
no.3
/
pp.218-231
/
2019
Background: We recently reported that Salvia plebeia R. Br. extracts suppress leukotriene production and effectively inhibit the airway inflammatory response by modulating inflammatory chemokine and cytokine expression. Here, we investigated the synergistic airway anti-inflammation effect of Salvia plebeia and Panax ginseng (Korean red ginseng, KRG) that has been used to treat various immune diseases such as asthma. Methods and Results: To evaluate the synergistic airway anti-inflammatory effect of Salvia plebeia and KRG, we measured the inhibitory effect of monotheraphy with either or co-theraphy with both on leukotriene and reactive oxygen species (ROS) production. Using coal a combustion, fly ash, and diesel exhaust particle (CFD)-induced respiratory disease mouse model, we found that co-theraphy synergistically suppressed airway inflammatory signs such as alveolar wall thickness and collagen fibers deposition, and decreased the number of total cell, $CD11b^+Gr-1^+$ cells, and inflammatory cytokines (IL17A, TNF, MIP-2 and CXCL-1) in bronchoalveolar lavage (BAL) fluid. Conclusions: We confirmed respiratory protection as a therapeutic effect of the Salbia plebeia-KRG 3 : 1 complex (KGC-03-PS) via anti-tracheal muscle contraction and expectorant animal studies using a CFD-induced respiratory disease mouse model.
We previously reported the potential of Senna tora L. seeds fermented by Lactobacillus casei (FSL) as a laxative agent in a loperamide-induced constipation rat model. Here, we examine the mechanism of action of FSL and its bioactive compound, revealed herein, on loperamide-induced constipation Sprague Dawley rat model. We identified the compound aurantio-obtusin (AO) using HPLC quantitative analysis. Rats were randomly assigned to six experimental groups (eight rats each)-normal and constipated groups (loperamide, FSL [100, 300, 500 mg/kg], and AO [1 mg/kg]). The FSL and AO-treated group showed an increase in the frequency, amount, and water content of feces in the constipated rat. Moreover, FSL and AO increased the intestinal transit speed in the constipated rat. Histological analysis revealed that FSL and AO recovered the intestinal mucus, the number of goblet cells, as well as thickness of the mucosa layer and muscle. Furthermore, the protein levels of the muscarinic acetylcholine receptor M3, which is involved in intestine contraction, were recovered in the FSL and AO-treated group. Its downstream signaling pathway (p-protein kinase C) was recovered by FSL and AO treatment. In conclusion, fermentation of S. tora L. seeds increases AO, which improves intestinal function, indicating that FSL is effective for treating constipation.
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