• Title/Summary/Keyword: blockers

Search Result 296, Processing Time 0.038 seconds

Analytic Formulation of Transmission Light Intensity of Hole Blockers in Intensity-based Polymer Optical Fiber Sensors

  • Kwon, Il-Bum;Kim, Chi-Yeop;Shim, Chan-Wook;Hwang, Du-Sun;Chung, Yung-Joo
    • Journal of Sensor Science and Technology
    • /
    • v.20 no.4
    • /
    • pp.221-225
    • /
    • 2011
  • Intensity-based optical fiber sensors are devised using a blocker which is located between two polymer optical fibers(POFs), one fiber is light-in and the other is light-out. This blocker is moved by an external displacement. Therefore, finding a general formulation of the relation between this displacement and transmission light intensity of various blockers is important to help develop intensity-based optical fiber sensors. In this paper, we consider blockers with arbitrary shapes from circular holes to inclined angled blockers. The transmission light intensities of such blockers should be determined by this generalized equation. In order to verify this equation, the calculated intensities of the blockers are compared with the values acquired from experiment. In the comparison, it is shown that the analytic equation can give the exact values of the transmitted light intensities for the assorted blockers. The range of the displacement measurement is also shown to be about 6 times of the radius of the hole in the case of a 9 degree inclined angle blocker.

Separation of the Enantiomers of β-Blockers Using Brush Type Chiral Stationary Phase Derived from Conformationally Rigid α-Amino β-Lactam

  • Pirkle, William H.;Lee, Won-Jae
    • Bulletin of the Korean Chemical Society
    • /
    • v.31 no.3
    • /
    • pp.620-623
    • /
    • 2010
  • A brush type chiral stationary phase (CSP 2) derived from ${\alpha}$-amino ${\beta}$-lactam was prepared for the separation of the enantiomers of ${\beta}$-blockers. Compared to the CSP derived from ${\alpha}$-amino phosphonate (CSP 1), in general, the conformationally rigid CSP 2 showed greater scope and much enhanced enantioselectivity for the resolution of ${\beta}$-blockers. The effect of various salt additives on enantioseparation of ${\beta}$-blockers in the mobile phase was investigated. The unusual effect of temperature on the chromatographic behaviors was observed on CSP 2. It also afforded appreciable increases in enantioselectivity without significantly affecting resolution, as the column temperature was reduced.

Are Beta Blockers New Potential Anticancer Agents?

  • Akbar, Shahid;Alsharidah, Mansour Saleh
    • Asian Pacific Journal of Cancer Prevention
    • /
    • v.15 no.22
    • /
    • pp.9567-9574
    • /
    • 2014
  • ${\beta}$-Blockers have been one of the most widely used and versatile drugs for the past half a century. A new potential for their use as anti-cancer drugs has emerged in the past few years. Various retrospective case control studies have been suggestive that use of ${\beta}$-blockers before the diagnosis of cancer could have preventive and protective effects against non-small cell lung carcinoma, melanoma, and breast, pancreatic and prostate cancers. Experimental and clinical observations are still inconclusive with some inconsistent findings. However, indications are pointing toward a positive role of some ${\beta}$-blockers against certain forms of cancers. This mini review is an effort to present the up to date published results of case-control studies and experimental findings.

Relative potency of antihistaminics for $H_1$-and muscarinic receptors (항 히스타민제의 $H_1$ 수용체와 무스카린 수용체에 대한 상대적 역가)

  • 이신웅;박영주;이정수
    • YAKHAK HOEJI
    • /
    • v.37 no.4
    • /
    • pp.397-407
    • /
    • 1993
  • The muscarinic antagonist l-[benzilic-4,4'-$^3H$]quinuclidinyl benzilate([$^3H$]QNB) bound to a single class of muscarinic receptor with high affinity in guinea pig ileal membranes. The $K_{D}$ and B$_{max}$ values for [$^3H$]QNB calculated from analysis of saturation isotherms were 54 pM and 156fmol/mg, respectively. H$_{1}$-blockers inhibited [$^3H$]QNB binding to ileal membranes with $K_{i}$ values ranged from 0.008 $\mu{M}$ to 1.6 $\mu{M}$. The pseudo-Hill coefficients of H$_{1}$-blockers for inhibition of [$^3H$]QNB binding to the ileal membranes were close to unit. The $K_{i}$ values for H$_{1}$-blockers were similar to the $K_{M}$ values calculated by Schild plot of functional data obtained from inhibition of the carbachol-induced contraction in guinea-pig ileum, suggesting that binding of H$_{1}$-blockers vs [$^3H$]QNB in ileal membranes represents an interaction with a receptor of physiological relevance. The $K_{H}$ values of H$_{1}$-blockers for H$_{1}$-receptor estimated from inhibition of the histamine-induced contraction were the range of 0.15 nM to 56.5 nM. The $K_{M}$/K$_{H}$ ratio of H$_{1}$-blockers varied over a wide range of 3 to 2300. Thus, the antihistaminic potencies of H$_{1}$-blockers do not correlate with their antimuscarinic potencies, which suggest that antihistamines have different antimuscarinic potencies in therapeutic blood levels causing similar antiallergic effect. Among 13 traditional antihistaminics examined in this study, drug having the highest and the lowest $K_{M}$/K$_{H}$ ratio is triprolidine and diphenidol, respectively. The present results demonstrate that the antimuscarinic property of antihistamines is not necessary for their antiallergic effect, and data on the affinity of antihistamines for muscarinic and H$_{1}$-receptors can be an important parameter in the selection and evaluation of these drugs.

  • PDF

Characterization of Adsorbents for the Simultaneous Solid-Phase Extraction of Trace $\beta$-Blockers from Biological Samples (생체시료로부터 미량 $\beta$-Blockers의 동시고상추출에 사용될 흡착제들의 특성)

  • Kim, Kyoung Rae;Kim, Do Jeong
    • Analytical Science and Technology
    • /
    • v.6 no.4
    • /
    • pp.375-381
    • /
    • 1993
  • The efficiencies of four different solid absorbents were evaluated for the simultaneous solid-phase extraction of six ${\beta}$-blockers from biological sample. Chromosorb 107 using methanol as the eluting solvent gave the highest solid-phase extraction yield. From the breakthrough studies of ${\beta}$-blockers, the excellent sorption and desorption properties of the Chromosorb 107 column were verified. The usefulness of Chromosorb 107/methanol was examined for the simultaneous solid-phase extraction of the ${\beta}$-blockers from serum in the concentration range of 2~8ppm.

  • PDF

Pharmacological Studies on the Antihypertensive Effects of Cinnarizine Coadministered with Propranolol or Metoprolol(III) -Effects on Biochemical Changes- (Cinnarizine을 Propranolol이나 Metoprolol과 병용할 때의 혈압강하효과(血壓降下效果)에 관한 약리학적(藥理學的) 연구(硏究)(III) -생화학적(生化學的) 변화(變化)에 대한 영향-)

  • Huh, In-Hoi;Ann, Hyung-Soo
    • YAKHAK HOEJI
    • /
    • v.28 no.5
    • /
    • pp.265-273
    • /
    • 1984
  • The effects of cinnarizine, $Ca^{2+}-antagonist$, on the antihypertensive effect of coadministered ${\beta}-blockers$, propranolol and metoprolol, were investigated in SHR. Drugs were coadministered orally for 4 weeks. Hemodynamic and biochemical changes induced by above drugs were determined to elucidate their mechanism of action. a) Cardiohypertropy of SHR was significantly improved by the treatment of ${\beta}-blockers$ as well as combination with cinnarizine and ${\beta}-blockers$. b) $Mg^{2+}-contents$ were increased in ventricle and decreased in plasma and aorta in all of the groups, especially in the group of propranolol with cinnarizine. c) c-GMP contents in ventricle were increased when cinnarizine was coadministered with propranolol, and c-GMP contents in aorta were increased when cinnarizine was coadministered with metoprolol, camparing with propranolol or metoprolol alone-treated group. d) Plasma renin activity appeared to be increased in cinnarizine treated alone, but reduced by combination with ${\beta}-blockers$. e) Triglycerides and $Na^+$ contents in serum were decreased in the group of metoprolol with cinnarizine, comparing with metoprolol alone-treated group. Increased $K^+\;and\;Ca^{2+}$excretions in urine by ${\beta}-blockers$ were inhibited by cinnarizine, so $Na^+/K^+$ excretion ratios were increased. Diuretic effects was showed in metoprolol alone treated group, but reduced when coadministered with cinnarizine.

  • PDF

Pharmacophore Modelling, Quantitative Structure Activity Relationship (QSAR) and Docking Studies of Pyrimidine Analogs as Potential Calcium Channel Blockers

  • Choudhari, Prafulla B.;Bhatia, Manish S.;Jadhav, Swapnil D.
    • Journal of the Korean Chemical Society
    • /
    • v.57 no.1
    • /
    • pp.99-103
    • /
    • 2013
  • The present communication deals with the Pharmacophore modeling, 3D QSAR and docking analysis on series of Pyrimidine derivatives as potential calcium channel blockers. The computational studies showed hydrogen bond donor, hydrogen bond acceptor, and hydrophobic group are important features for calcium channel blocking activity. These studies showed that Pyrimidine scaffold can be utilized for designing of novel calcium channels blockers for CVS disorders.

Chiral separation of $\beta$-blockers after derivatizalion wilh a new chiral derivalizalion agen1.GATC and Comparison wilh GITC on derivalizing conditions and chromalographic paramelers

  • Ko, Mi-Young;Shin, Dae-Hong;Seo, Sang-Hun;Kim, Kyeong-Ho
    • Proceedings of the PSK Conference
    • /
    • 2002.10a
    • /
    • pp.398.1-398.1
    • /
    • 2002
  • A new chiral derivatization agent with sugar moiety. 2, 3.4, 6-tetra-O-acetyl-D-galactopyranosyl isothiocyanate (GATC) was synthesized. Several $\beta$-blockers were investigated for the possible separation of the enantiomers by reversed-phase HPLC after derivatization with this new chiral derivatization agent (GATC). GATC was reacted readily with $\beta$-blockers at room temperature and the reaction mixture could directly be injected into the HPLC system. (omitted)

  • PDF

Analysis of $\beta$-blockers Use in Chronic Heart Failure

  • Kang, Hyo-Jin;Lee, Suk-Hyang
    • Proceedings of the PSK Conference
    • /
    • 2003.10b
    • /
    • pp.249.2-250
    • /
    • 2003
  • ${\beta}$-blockers are considered as standard therapy for patients with stable chronic heart failure (CHF) and to prolong survival and reduce hospitalizations. We examined the effects of the ${\beta}$-blocker on mortality, hospitalization and symptoms in patients with CHF and the related factors to the use of ${\beta}$-blockers. Patients in New York Heart Association class II-IV were included if they were treated for heart failure from January 2002 to June 2002. At baseline, 6 months, and 12 months, they were assessed for the change of NYHA class and all deaths and hospital admissions. (omitted)

  • PDF

Chiral Separation of ${\beta}-Blockers$ after Derivatization with a New Chiral Derivatization Agent, GATC

  • Ko, Mi-Young;Shin, Dae-Hong;Oh, Joung-Weon;Asegahegn, Workaferhaw Shibru;Kim, Kyeong-Ho
    • Archives of Pharmacal Research
    • /
    • v.29 no.11
    • /
    • pp.1061-1065
    • /
    • 2006
  • A new chiral derivatization agent with sugar moiety, 2,3,4,6-tetra-O-acetyl-${\beta}$-D-galactopyranosyl isothiocyanate (GATC) was synthesized. Several ${\beta}-blockers$ were investigated for the possible separation of the enantiomers by reversed-phase HPLC after derivatization with this new chiral derivatization agent (GATC). GATC was reacted readily with ${\beta}-blockers$ at room temperature and the reaction mixture could directly be injected into the HPLC system. The corresponding diastereomers were well resolved on an ODS column with acetonitrile-ammonium acetate buffer as a mobile phase and monitored at UV 254 nm. The optimization of the derivatization procedure (concentration of GATC, reaction temperature and time) and HPLC conditions (pH and ionic strength of mobile phase) were investigated and compared with GITC.