• Title/Summary/Keyword: Adrenergic alpha-1 receptor

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Effects of opioid and non-opioid antagonists, pH and enzymes on Corchorus olitorius antinociception in mice

  • Zakaria Zainul Amiruddin;Neelendran M;Pubalan S;Sulaiman MR;Fatimah CA
    • Advances in Traditional Medicine
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    • v.6 no.3
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    • pp.186-195
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    • 2006
  • The present study was carried out to determine the involvement of opioid and non-opioid receptor and the effect of pH and enzymes on the recently reported antinociceptive activity of aqueous extract of Corchorus olitorius (AECO) leaves using the abdominal constriction test. The extract was prepared by soaking the dried powdered leaves of Corchorus (C.) olitorius in distilled water overnight, and the supernatant obtained was considered as a stock solution with 100% concentration/ strength. The extract, administered subcutaneously in the concentrations/ strength of 10, 50 and 100%, was found to show a significant concentration-independent antinociception. The 50% concentration AECO were further used to study on the above mentioned parameters. The extract exhibited: significant (P < 0.05) decreased in activity when pre-treated (s.c.) against 10 mg/kg naloxonazine, bicuculine (10 mg/kg), phenoxybenzamine (10 mg/kg), 10 mg/kg pindolol, and 5 mg/kg mecamylamme, but not 10 mg/kg naltrindole, 10 mg/kg atropine, respectively; significant (P < 0.05) decreased in activity after pre-treatment against 10% a-amylase, but not 1 % protease or 10% lipase and; significant (P < 0.05) decreased in activity after exposure to alkaline condition (pH between 9 and 13) while maintaining the activity at acidic condition, respectively. The C. olitorius leaves antinociception, which involved, at least in part, activation of $\mu-opioid,\;\alpha-and\;\beta-adrenergic$, and nicotinic receptors, was found to decrease under alkaline condition and in the presence of $\alpha-amylase$.

Influence of Ginseng Saponins on the Isolated Aortic Contractile Response of the Spontaneously Hypertensive Rat

  • Lim, Dong-Yoon;Cha, Dong-Seok
    • Journal of Ginseng Research
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    • v.26 no.4
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    • pp.178-186
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    • 2002
  • The present study was attempted to investigate the effects of total ginseng saponin (G75), panaxadiol-type (PDS) and panaxatriol-type saponin (PTS) on contractile responses of vasoconstrictors in aortic smooth muscle stripes of normotensive (NR) and spontaneous hypertensive rats (SHR). Phenylephrine (an adrenergic $\alpha$$\_$1/-receptor agonist) and high potassium (a membrane depolarizing agent) caused greatly contractile responses in both NR and AHR aorta, respectively. Phenylephrine- and high potassium-induced contractile responses were greater in NA than those in SHR aortic smooth muscle stripes. In NR, the contractile responses of high potassium (5.6$\times$10$\^$-2/ M) were not affected in the presence of GTS (300 $\mu$g/ml), PDS (300 $\mu$g/ml), and PTS (300 $\mu$g/ml), respectively whereas phenylephrine (10$\^$-6/ M)-induced contractile responses were markedly inhibited. In SHR, the contractile responses of high potassium (5.6$\times$10$\^$-2/ M) were not affected in the presence of GTS (300 $\mu$g/ml), PDS (300 $\mu$g/ml), and moderate doses of PTS (150-300 $\mu$g/ml), respectively but greatly blocked by high concentration of PTS (600 $\mu$g/ml). Phenylephrine (10$\^$-6/ M)-induced contractile responses were inhibited in a dose dependent fashion (150-600 $\mu$g/ml) by the pretreatment with PTS while not altered in the presence of GTS (300 $\mu$g/ml) and PDS (300 $\mu$g/ml), respectively. Taken together, these experimental results suggest that ginseng saponins cause vascular relaxation through blockade of adrenergic $\alpha$$\_$1/-receptors and some unknown mechanisms, and that there is some difference in sensitivity of vascular smooth muscle between NR and SHR in responses to ginseng saponins. It seems that panaxatriol type of some ginseng saponins has the greatest potency in vascular relaxation.

Effects of frequency - amplitude electrical stimulation on sympathetic neurotransmitter and vasoactive intestinal peptide (SSP 주파수 진폭변조가 Vasoactive Intestinal Peptide와 $\beta$-endorphin, cGMP에 미치는 영향)

  • Choi Young-duk;Shim Kyu-Rhee;Chang Moon-kyung
    • The Journal of Korean Physical Therapy
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    • v.14 no.4
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    • pp.454-474
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    • 2002
  • Vasoactive intestinal peptide (VIP) is a very potent dilatator and a nonadrenergic, noncholinergic (NANC) neurotransmitter or neuromodulator in the peripheral and the central nervous systems. The mechanisms of action of VIP were examined in aortic circular and in uterine longitudinal smooth muscle strips of the rat. The effects of sympathetic neurotransmitter were investigated in gastric and aortic circular muscle strips of the mouse and the rat. The effects of silver spike point, SSP, low frequency electrical stimulations of VIP, sympathetic neurotransmitter and $\beta$-endorphin were examined in plasma, serum and 24h urine from the healthy volunteer. In gastric smooth muscle strips from the mouse, adrenergic neurotransmitter norepinephrine was inhibitory effected, followed by caused phasic and tonic contraction to the, muscrine receptor agonist carbachol and acetylcholine, respectively. In urine from the healthy volunteer, both norepinephrine and epinephrine were significantly decreased in continue type and low frequency (3 Hz) of SSP electrical stimulations. The contractile responses to S-HT in uterine longitudinal smooth muscle strips of the rats were completely decreased by a VIP 1 $\mu$M. The contractile responses to PGF2$\alpha$ were not decreased by a VIP. In plasma and serum from the healthy volunteer, both VIP and $\beta$-endorphin were significantly increased in continue type and low frequency (3 Hz) of SSP electrical stimulations. Therefore, this study demonstrate that VIP has the capacity to relax vascular or gastric smooth muscles in part by stimulating the generation of NO, and silver spike point low frequency electrical stimulation has the capacity both to decrease sympathetic neurotransmitters and to increase VIP, $\beta$-endorphin.

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Meta-analysis of the Korean Literatures for Developing Clinical Practice Guidelines of Benign Prostatic Hyperplasia (전립선비대증의 진료지침 개발을 위한 한국문헌의 메타분석)

  • Yu, Seung-Hum;Kim, Chun-Bae;Kang, Myung-Geun;Song, Jae-Mann
    • Journal of Preventive Medicine and Public Health
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    • v.30 no.3 s.58
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    • pp.643-664
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    • 1997
  • This study is to provide evidence-based recommendations for the most-effective treatments of benign prostatic hyperplasia based on patient preference or clinical need, and to meta-analyze the Korean literatures for the development of BPH treatment guidelines. For these analyses, extensive literature searches (208 articles), with priority given to the Korean Journal of Urology, were conducted from 1960 to August, 1996. Meta-analysis, like all statistical analysis, has two main functions: data summarization (qualitative meta-analysis) and smoothing o. pattern recognition (quantitative meta-analysis). As well, critical reviews and syntheses with the mean and 90-percent confidence intervals for the likelihood were used to evaluate empirical evidence and significant outcomes of the BPH treatment literatures (106 articles). For this task, the Methodologic Panel for BPH Guidelines was composed of multidisciplinary experts in the field. The results of the study were summarized as follows: For all that watchful waiting is an appropriate treatment strategy for the majority of patients with prostatism, we couldn't find the Korean literatures which carried this article. The literatures on alpha-1-adrenergic receptor blockers provide no evidence to suggest that any one alpha blocker is more effective than another. The finasteride reduces the size of the prostate, on average, and leads to a small yet perceptible reduction in sysptoms. Of all treatment options, prostate surgery with transurethral resection of the prostate (TURP), transurethral incision of the prostate (TUIP), and so on, offers the best chance for symptom improvement. However, surgery also has the highest rates of significant complications. Therefore, surgery need not always be a treatment of last resort. Balloon dilation of the prostatic urethra is clearly less effective than surgery in relieving symptoms, but it is associated with fewer complications. Emerging technologies for treating BPH include lasers, coils, stents, thermal therapy and hyperthermia. Established technologies will also be reanalyzed as results of new trials are reported. Although this study has some limitations due to lacking for good quality literatures, ' it provides a cornerstone for our medical research. It represents the most current scientific knowledge regarding the clinical epidemiology including treatment of BPH. It will be revised and updated as needed.

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Influence of Blockade of Sympathetic Nervous System, Renin-Angiotensin System, and Vasopressin System on Basal Blood Pressure Levels and on Pressor Response to Norepinephrine, Angiotensin II, and Vasopressin (교감신경계, Renin-Angiotensin계, Vasopressin계의 차단이 혈압 및 Norepinephrine, Angiotensin II 및 Vasopressin의 승압효과에 미치는 영향)

  • Chung, Haeng-Nam
    • The Korean Journal of Pharmacology
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    • v.28 no.1
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    • pp.61-74
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    • 1992
  • Influence of the blockade of the three major pressor systems-sympathetic nervous system (SNS), renin-angiotensin system (RAS) and vasopressin system-on the pressor responsiveness to norepinephrine (NE), angiotensin II (AII), and vasopressin (VP) as well as on basal blood pressure (BP) levels was investigated in urethane-anesthetized rabbits. To block the SNS and RAS, chlorisondamine (CS) and pirenzepine (PZ), sympathetic ganglionic blockers, and enalapril (ENAL), an inhibitor of angiotensin converting enzyme, respectively were used. And for suppressing the VP system bremazocine (BREM), a kappa opiate receptor agonist shown to suppress plasma levels of VP, was employed. Each of CS (0.4 mg/kg), ENAL (2 mg/kg), and BREM (0.25 mg/kg) produced almost same levels of steady hypotensive state. The hypotensive effect of BREM was significantly attenuated by desmopressin, a synthetic VP-like analogue, suggesting the hypotension being at least in part due to suppression of plasma levels of VP. CS, ENAL and BREM elicited further fall of the BP which had been lowered by ENAL or BREM, CS or BREM, and CS or ENAL, respectively. The hypotension produced by both CS and PZ together with either of ENAL or BREM was more marked than that produced by the three drugs other than CS. CS potentiated the pressor response not only to NE but to AII and VP. The pressor effect of AII was increased by ENAL and BREM, too. The pressor response to VP was also enhanced by BREM. Blockade of ${\alpha}-adrenergic$ receptors with phentolamine or phenoxybenzamine potentiated the pressor response to AII and that to VP. The results on basal BP levels indicate that the three major pressor systems are all participating in control of BP, but SNS has the greatest potential for supporting BP. The finding that blockade of one of the pressor systems induced enhanced pressor responsiveness to the pressor hormone of that particular system as well as to the pressor hormone(s) of the other systems(s) provides evidence for important interactions among the three major pressor systems.

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