• Title/Summary/Keyword: NECA

Search Result 35, Processing Time 0.02 seconds

Influence of 5′-(N′-Ethylcarboxanlido) Adenosine on Catecholarnine Secretion Evoked by Cholinergic Stimulation and Membrane Depolarization in the Rat Adrenal Gland

  • Lim, Dong-Yoon;Oh, Hyeong-Geun;Woo, Seong-Chang
    • Biomolecules & Therapeutics
    • /
    • v.8 no.4
    • /
    • pp.338-348
    • /
    • 2000
  • The present study was attempted to determine the effect of 5'-(N'-ethylcarboxamido) adenosine (NECA), which is an potent $A_2$-adenosine receptor agonist, on catecholamine (CA) secretion evoked by cholinergic stimulation, membrane depolarization and calcium mobilization from the isolated perfused rat adrenal gland. NECA (20 nM) perfused into the adrenal vein for 60 min produced a time-related inhibition in CA secretion evoked by ACh (5.32x10$^{-3}$ M), high $K^{+}$(5.6x10$^{-2}$ M), DMPP (10$^{-4}$ M for 2 min), McN-A-343 (10$^{-4}$ M for 2 min), cyclopiazonic acid (10$^{-5}$ M for 4 min) and Bay-K-8644 (10$^{-5}$ M for 4 min). Also, in the presence of $\beta$,${\gamma}$-methylene adenosine-5'-triphosphate (MATP), which is also known to be a selective $P_{2x}$-purinergic receptor agonist, showed a similar inhibition elf CA release evoked by ACh, high potassium, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid. However, in adrenal glands preloaded with 20$\mu$M NECA for 20 min under the presence of 20$\mu$M 3-isobutyl-1-methyl-xanthine (IBMX), an adenosine receptors antagonist, CA secretory responses evoked by ACh, high potassium, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid were much recovered in comparison to the case of NECA-treatment only. Taken together, these results indicate that NECA causes the marked inhibition of CA secretion evoked by stimulation of cholinergic (both nicotinic and muscarinic) receptors as well as by membrane depolarization. This inhibitory effect may be mediated by inhibiting influx of extracellular calcium and release in intracellular calcium in the rat adrenomedullary chromaffin cells through the adenosine receptor stimulation. Therefore, it is suggested that the inhibitory mechanism of adenosine receptor stimulation may play a modulatory role in regulating CA secretion.n.n.

  • PDF

Receptor Specificity of Adenosine Analogs in Terms of Renal Function and Renin Release (Adenosine 유사체의 신장효과에 미치는 Adenosine 차단제의 영향)

  • Yun, Young-Yi;Koh, Gou-Young;Kim, Suhn-Hee;Cho, Kyung-Woo
    • The Korean Journal of Physiology
    • /
    • v.24 no.2
    • /
    • pp.269-280
    • /
    • 1990
  • The purpose of the present experiment was to determine the functional subclassification of renal adenosine receptor fer the hemdynamic, excretory and secretory functions in unanesthetized rabbits. Adenosine antagonist, 8-phenyltheophylline (8-PT) or theophylline, was infused into the left renal artery followed by an infusion of adenosine agonist, cyclohexyladenosine (CHA) or 5'-N-ethylcarboxamidoadenosine (NECA). Intrarenal arterial infusion of CHA or NECA caused decreases in urine volume, glomerular filtration rate, renal plasma flow and excreted amount of electrolytes and renin release in a dose-dependent manner. Dose-response curves in renal function by CHA or NECA was similar and shifted to the right with pretreatment of 8-PT or theophylline. No significant differences in renal response to CHA and NECA in antagonist-treated rabbits were observed. However, the decrease in renin secretion rate was not affected by the adminstration of adenosine antagonists. These results suggest that the renal effect of adenosine receptor agonists appears by way of specific adenosine receptor, but which is not functionally subclassified in the rabbit.

  • PDF

Effect of Adenosine Analogues on the Renal Function and Renin Release (가토의 신장기능과 Renin분비에 미치는 Adenosine Analogues의 영향)

  • Song, Yun-Sik;Choi, Byung-Soo;Kim, Suhn-Hee;Cho, Kyung-Woo
    • The Korean Journal of Physiology
    • /
    • v.22 no.2
    • /
    • pp.319-332
    • /
    • 1988
  • The regulations of renal function and renin release are influenced by neural, humoral and physical factors. During the last decade, considerable progress has been made in the identification and characterization of these extrinsic renal control systems. Mechanisms intrinsic to the kidney are also important for renal function. These include the autoregulation of blood flow, and the local control of renin secretion. Fundamental questions regarding the mechanism of these intrinsic controls remain unanswered. Recently, endogenous renal adenosine has been claimed to influence the tubuloglomerular feedback control and renin release. Two subclasses of adenosine receptors $A_1{\;}and{\;}A_2$ have been described. The present experiment was carried out to evaluate the effects of $N_6-cyclohexyladenosine$ $(CHA,{\;}A_1{\;}selective)$ and 5'-N-ethylcarbox-amide adenosine $(NECA,{\;}A_2{\;}selective)$ on the renal function and renin release in the unanesthetized rabbit. Intra-renal arterial infusion of NECA $(0.3{\sim}10.0n{\;}mole/min/rabbit)$ or CHA $(0.03{\sim}10.0n{\;}mole/min/rabbit)$ caused a prompt and dose-dependent decrease in urine volume, glomerular filtration rate (GFR), renal plasma flow (RPF), filtration fraction (FF), electrolyte excretion and free water clearance $(CH_2O)$, the effect being much more profound with CHA than with NECA. The NECA infusion resulted in a profound decrease of systemic blood pressure, but the CHA infusion did not. Both NECA and GHA infusions caused a prompt and dose-dependent decrease in renin secretion rate, again the effect being greater with CHA than with NEGA. These results suggest that both $A_1{\;}and{\;}A_2$ adenosine receptors may be involved in the intrinsic control of renal function and renin release, and that the $A_1$ receptors plays a more important role than the $A_2$ receptor in the regulation of renal fnction.

  • PDF

The Development and Effect of Doctor-Visiting Nurses ICT Communication System for the Elderly: Focusing on Visiting Nursing Services for Long-term Care Patients (고령자 대상 의사-의료인간 ICT활용 협진 모델개발 및 실증에 관한 연구: 장기요양서비스 중 재가노인대상 방문간호서비스를 중심으로)

  • Cha, Sunmi;Yoo, Keunjoo;Choi, Solji;Hong, Seokwon
    • Journal of Korean Gerontological Nursing
    • /
    • v.20 no.sup1
    • /
    • pp.137-143
    • /
    • 2018
  • Purpose: The purpose of this study was to examine effectiveness and usefulness of Information Communication Technology (ICT) in communication between physician and visiting nurses who provide visiting nursing services under long-term care insurance. Methods: Structured questionnaires were used to measure usefulness and satisfaction of the system, both accessibility and convenience to visiting nurses (31 people) and users (182 people). Results: From the user perspective, accessibility and convenience in terms of service users were both satisfactory as shown by users' percentage. No statistically significant difference was found for satisfaction between before and after using the system. The usefulness of the system for visiting nurses was satisfactory for most the nurses. Also most nurses answered that the system is needed and is very useful. Most of the participants (both visiting nurse and service users) were satisfied with use of the ICT system. However, there was no statistically significant difference in satisfaction between the pre and post service because the service provision period was too short (three months). Conclusion: The consensus from both users and service providers is that an ICT based visiting nursing system needs to be introduced but a more user - friendly environment for system development will be needed.

Effects of Cyclic Nucleotides on the Cerebral Blood Row Response Induced by Adenosine A2B Receptor Agonist in the Rats

  • Kim, Hyun-Seung;Shin, In-Chul
    • Biomolecules & Therapeutics
    • /
    • v.12 no.2
    • /
    • pp.108-113
    • /
    • 2004
  • This study was performed to investigate the regulatory mechanism of cerebral blood flow of adenosine $A_{2B}$ receptor agonist in the rats, and to define whether its mechanism is mediated by adenylate cyclase and guanylate cyclase. in pentobarbital-anesthetized, pentobrabital-paralyzed and artificially ventilated male Sprague-Dawley rats, all drugs were applied topically to the cerebral cortex. Blood How from cerebral cortex was measured using laser-Doppler flowmetry. Topical application of an adenosine $A_{2B}$ receptor agonist, 5'-N-ethylcar-boxamidoadenosine (NECA; 4 umol/l) increased cerebral blood flow. This effect of NECA (4 umol/l) was not blocked by pretreatment with adenylate cyclase inhibitor, MDL-12330 (20 umol/l). But effect of NECA (4 umol/l) was blocked by pretreatment with guanylate cyclase inhibitor, LY-83383 (10 umol/l). These results suggest that adenosine $A_{2B}$ receptor increases cerebral blood flow. It seems that this action of adenosine $A_{2B}$ receptor is mediated via the activation of guanylate cyclase in the cerebral cortex of the rats.

Effects of Adenylate Cyclase, Guanylate Cyclase and KATP Channel Blockade on the Cerebral Blood Flow Response Induced by Adenosine A2B Receptor Agonist in the Rats

  • Youn, Doo-Sang;Shin, In-Chul
    • Biomolecules & Therapeutics
    • /
    • v.13 no.1
    • /
    • pp.35-40
    • /
    • 2005
  • This study was performed to investigate the regulatory mechanism of cerebral blood flow of adenosine A$_{2B}$ receptor agonist in the rats, and to define whether its mechanism is mediated by adenylate cyclase, guanylate cyclase and potassium channel. In pentobarbital-anesthetized, pancuronium-paralyzed and artificially ventilated male Sprague-Dawley rats, all drugs were applied topically to the cerebral cortex. Blood flow from cerebral cortex was measured using laser-Doppler flowmetry. Topical application of an adenosine A$_{2B}$ receptor agonist, 5'-N-ethylcarboxamidoadenosine (NECA; 4 umol/I) increased cerebral blood flow. This effect of NECA (4 umol/I) was not blocked by pretreatment with adenylate cyclase inhibitor, MDL-12,330 (20 umol/I). But effect of NECA (4 umol/I) was blocked by pretreatment with guanylate cyclase inhibitor, LY-83,583 (10 umol/I) and pretreatment with ATP-sensitive potassium channel inhibitor, glipizide (5 umol/I). These results suggest that adenosine A$_{2B}$ receptor increases cerebral blood flow. It seems that this action of adenosine A$_{2B}$ receptor is mediated via the activation of guanylate cyclase and ATP-sensitive potassium channel in the cerebral cortex of the rats.

Renal Effects of Chronic Treatment Of Adenosine Analogues (Adenosine 수용체 작동제 장기 투여의 신장효과)

  • Kim Tack-Hee;Kim Suhn-Hee;Huh Jong;Cho Kyung-Woo
    • The Korean Journal of Physiology and Pharmacology
    • /
    • v.1 no.3
    • /
    • pp.325-335
    • /
    • 1997
  • Evidence for the existance of at least two subclasses of renal adenosine receptors has been presented. N-6-cyclohexyladenosine (CHA) is a relatively selective $A_1$ adenosine agonists, whereas 5'-N-ethylcarboxamidoadenosine (NECA) acts as a preferential agonist of $A_2$ adenoisne receptor. N6-(L-2-phenylisoproryl)-adenosine (PIA) almost unselectively activates both $A_1\;and\;A_2$ adenosine receptors at micromolar concentrations. During the characterization of adenosine receptor in the kidney, we have discovered a novel phenomenon, that is, an intramuscular administration of CHA for 3 days caused a diuresis and a suppression of urinary concentrating ability. To further characterize this novel phenomenon, an intramuscular administration of adenosine and other adenosine angonists, PIA and NECA, and prior treatment of adenosine antagonists, caffeine, theophylline and 1,3-diethyl-8-phenyl-xanthine (DPX) were performed. Systemic administration of CHA, PIA, and NECA for 3 days caused a suppression in heart rate, blood pressure and general motor activity without change in rectal temperature. Systemic administration of CHA, 0.5, 1 and 2 mg/kg/day, for 3 days caused a dose-dependent increase in urine volume and decrease in urinary osmolarity and free water reabsorption. This phenomenon was reversible and repeatable. Administration of adenosine (40 mg/kg/day) produced no apparent effect on the renal function, whereas PIA (2 mg/kg/day) produced an similar effect to CHA on the renal function. Systemic adminstration of NECA, 0.025, 0.05 and 0.25 mg/kg/day, for 3 days caused a dose-dependent increase in urine volume and dose-dependent increases in excreted amount of creatinine, urinary osmolarity and free water reabsorption. These renal effects of adenosine agonist were maximum at second day during the drug administration. In terms of increase in urine volume and the suppression of urinary concentrating ability, NECA was potent than CHA. Prior treatment of caffeine (50 mg/kg/day) or theophylline (50 mg/kg/day) abolished the diuretic effect of CHA, whereas DPX (50 mg/kg/day) did not affect the CHA effect. CHA, 0.5 mg/kg/day, produced no change in plasma renin activity and plasma levels of aldosterone, epinephrine, and norepinephrine. These results suggest that this novel phenomenon produced by an activation of renal adenosine receptors plays an important role in urinary concentrating mechanism.

  • PDF

Prognostic Value of HPV18 DNA Viral Load in Patients with Early-Stage Neuroendocrine Carcinoma of the Uterine Cervix

  • Siriaunkgul, Sumalee;Utaipat, Utaiwan;Suwiwat, Supaporn;Settakorn, Jongkolnee;Sukpan, Kornkanok;Srisomboon, Jatupol;Khunamornpong, Surapan
    • Asian Pacific Journal of Cancer Prevention
    • /
    • v.13 no.7
    • /
    • pp.3281-3285
    • /
    • 2012
  • Objectives: To evaluate the clinicopathologic correlation and prognostic value of HPV18 DNA viral load in patients with early-stage cervical neuroendocrine carcinoma (NECA). Methods: Formalin-fixed, paraffin-embedded tissue of cervical NECA patients with known HPV18 infection and clinicopathologic data including follow-up results were collected. The HPV18 DNA load was assessed with quantitative PCR targeting the HPV18 E6E7 region. Results: Twenty-one patients with early-stage (IB-IIA) cervical NECA were identified. HPV18 DNA viral load ranged from 0.83 to 55,174 copies/cell (median 5.90). Disease progression, observed in 10 cases (48%), was not significantly associated with any clinicopathologic variables. However, the group of patients with progressive disease tended to have a higher rate of pelvic lymph node metastasis (50% versus 9%, p=0.063) and a lower median value of HPV18 DNA viral load (4.37 versus 8.17 copies/cell, p=0.198) compared to the non-recurrent group. When stratified by a cut-off viral load value of 5.00 copies/cell, the group of patients with viral load ${\leq}5.00$ copies/cell had a significantly shorter disease-free survival than the group with viral load >5.00 copies/cell (p=0.028). The group with a lower viral load also tended to have a higher rate of disease progression (75% versus 31%, p=0.080). No significant difference in the other clinicopathologic variables between the lower and higher viral load groups was identified. Conclusion: HPV18 DNA viral load may have a prognostic value in patients with early-stage NECA of the cervix. A low viral load may be predictive of shortened disease-free survival in these patients.

The Involvement of Nitric Oxide and Guanylate Cyclase on the Adenosine A2B Receptor-induced Cerebral Blood Responses in the Rats

  • Park, Chan-Sook;Shin, In-Chul
    • Biomolecules & Therapeutics
    • /
    • v.13 no.2
    • /
    • pp.95-100
    • /
    • 2005
  • This study was performed to investigate the mechanism of cerebral blood flow of adenosine $A_{2B}$ receptor agonist in the rats, and to define whether its mechanism is mediated by nitric oxide (NO) and guanylate cyclase. In pentobarbital-anesthetized, pancuronium-paralyzed and artificially ventilated male Sprague-Dawley rats, all drugs were applied topically to the cerebral cortex. Blood flow from cerebral cortex was measured using laser-doppler flowmetry. Topical application of an adenosine $A_{2B}$ receptor agonist, 5'-N-ethylcar-boxamidoadenosine (NECA; $4{\mu}mol/l$) increased cerebral blood flow. This effect of NECA ($4{\mu}mol/l$) was blocked by pretreatment with NO synthase inhibitor, $N^G$-nitro-L-argine methvlester (L-NAME; $40{\mu}mol/l$) and guanylate cyclase inhibitor, LY-83,583 ($10{\mu}mol/l$). These results suggest that adenosine $A_{2B}$ receptor increases cerebral blood flow. It seems that this action of adenosine $A_{2B}$ receptor is mediated via the NO and the activation of guanylate cyclase in the cerebral cortex of the rats.

Roles of Health Technology Assessment for Better Health and Universal Health Coverage in Korea (우리나라 보건의료 발전을 위한 의료기술평가의 역할)

  • Lee, Young Sung
    • Health Policy and Management
    • /
    • v.28 no.3
    • /
    • pp.263-271
    • /
    • 2018
  • Health technology assessment (HTA) is defined as multidisciplinary policy analysis to look into the medical, economic, social, and ethical implications of the development, distribution, and use of health technology. Following the recent changes in the social environment, there are increasing needs to improve Korea's healthcare environment by, inter alia, assessing health technologies in an organized, timely manner in accordance with the government's strategies to ensure that citizens' medical expenses are kept at a stable level. Dedicated to HTA and research, the National Evidence-based Healthcare Collaborating Agency (NECA) analyzes and provides grounds on the clinical safety, efficacy, and economic feasibility of health technologies. HTA offers the most suitable grounds for decision making not only by healthcare professionals but also by policy makers and citizens as seen in a case in 2009 where research revealed that glucosamine lacked preventive and treatment effects for osteoarthritis and glucosamine was subsequently excluded from the National Health Insurance's benefit list to stop the insurance scheme from suffering financial losses and citizens from paying unnecessary medical expenses. For the development of HTA in Korea, the NECA will continue exerting itself to accomplish its mission of providing policy support by health technology reassessment, promoting the establishment and use of big data and HTA platforms for public interest, and developing a new value-based HTA system.