• Title, Summary, Keyword: rat ileum

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Antimuscarine-like Action of Licorice Alkaloidal Fraction on Intestinal Smooth Muscle -Studies of Alkaloid of Glycyrrhiza glabra L. III- (감초(甘草) Alkaloidal Fraction 의 평활근(平滑筋)에 대(對)한 Acetylcholine 길항작용(拮抗作用) -감초 알카로이드에 관한 연구 (제 3 보)-)

  • Kim, Myung-Suk;Oh, Jin-Sup;Hong, Sa-Ack
    • The Korean Journal of Pharmacology
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    • v.5 no.2
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    • pp.121-127
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    • 1969
  • Antimuscarinic agent like antispasmodic actions of licorice alkaloidal fraction, obtained from the Glycyrrhiza glabra L., was compared with that of atropine quantitatively. For this purpose, the author calculated the kinetic constants and $ED_{50}$ for acetylcholine antagonism by these drugs on rat ileum and guinea-fig ileum longitudinal muscle according to Paton's theoretical equations describing the combination of an antagonist drug with its receptors. The results are as follows. 1. On rat ileum. a) Licorice alkaloidal fraction $K_1$ (association rate constant)=$4.078{\times}10^2\;(s^{-1}\;gm^{-1}\;ml)$ $K_2$ (dissociation rate constant)=$6.986{\times}10^{-4}\;(s^{-1})$ $ED_{50}(K_2/K_1)=1.772{\times}10^{-6}(gm/ml)$ b) Atropine $K_1=5.136{\times}10^6$, $K_2=7.714{\times}10^{-4}$, $ED_{50}=1.408{\times}10^{-10}$ 2. On guinea-pig ileum longitudinal muscle a) Licorice alkaloidal fraction $K_1=1.30{\times}10^2$, $K_2=1.25{\times}10^{-3}$ $ED_{50}=9.58{\times}10^{-6}$ b) Atropine $K_1=5.75{\times}10^6$, $K_2=1.54{\times}10^{-3}$ $ED_{50}=2.68{\times}10^{-10}$ Above results present that 1 r of licorice alkaloidal fraction has equal fotency of acetylcholine antagonism with $8.5{\times}10^{-5}r$ of atropine on rat ileum, $2.8{\times}10^{-5}r$ on guinea-pig ileum longitudinal muscle. This facts suggest that the site and numbers of licorice alkaloid receptors of guinea-pig ileum are different from that of rat ileum. Besides, it also gives a suggestion that licorice alkaloidal fraction may be a partial antagonist on guinea-pig ileum in this experimental conditions.

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The Screening of Biologically Active Plants in Korea Using Isolated Organ Preparation (IV) -Anticholinergic and Oxytocic Actions in Rat's Ileum and Uterus- (적출장기표본(摘出臟器標本)에 의한 국산생약(國産生藥)의 생리활성(生理活性) 검색(檢索) (IV) -흰쥐의 회장(回腸) 또는 자궁(子宮)에서의 항(抗)Acetylcholine 및 Oxytocin작용(作用)-)

  • Lee, Eun-Bang
    • Korean Journal of Pharmacognosy
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    • v.13 no.3
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    • pp.99-101
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    • 1982
  • The methanolic extracts of thirty-one medicinal plants were screened for anticholinergic and oxytocic activity in rat's ileum and uterus, respectively. In addition, their effects on the ileum and antagonism against oxytocin in the uterus were observed.

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Comparison of Gastrointestinal Permeability of Caffeine, Propranolol, Atenolol, Ofloxacin, and Quinidine Measured Using Ussing Chamber System and Caco-2 Cell Monolayer

  • Song, Im-Sook;Choi, Young A;Choi, Min-Koo
    • Mass Spectrometry Letters
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    • v.8 no.2
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    • pp.34-38
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    • 2017
  • The purpose of this study was to develop a cocktail approach for the measurement of the permeability of marker compounds, caffeine and propranolol (high permeability), ofloxacin (intermediate), atenolol (low), and quinidine (P-glycoprotein substrate), simultaneously. Then we compared the permeability in Caco-2 cells with that in rat intestinal segments. The difference between individual measurement and cocktail approach was less than 20 %, and the permeabilities of these compounds were similar to those previously reported, suggesting that the cocktail transport study and simultaneous drug analysis were successfully developed and validated in this study. Additionally, in the application of this cocktail method, the permeability of five drugs in rat jejunum was similar to that in ileum but different from that in colon, which was measured using the Ussing chamber system. Moreover, permeability in jejunum and ileum was similar to that in Caco-2 cells. In conclusion, the permeability in Caco-2 cells was equivalent to the permeability in rat jejunum and ileum determined with the Ussing system. Therefore, this newly developed cocktail assay and its application to the Ussing system can be a useful tool for robust and rapid screening for site-specific permeability in rat intestine, thus accelerating the prediction of absorption of new chemical entities.

Effect of Alisols Isolated from Alisma orientale Jazep. Against Several Agonists in Isolated Rat Ileum (택사의 Alisol성분들이 몇가지 Agonist에 의한 적출장관 수축에 미치는 영향)

  • YunChoi, Hye-Sook;Chung, Sung-Hyun;Kim, Young-Sook
    • Korean Journal of Pharmacognosy
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    • v.12 no.4
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    • pp.200-202
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    • 1981
  • Alisol B(II) and alisol B monoacetate (III) isolated from the rhizome of Alisma orientale Jazepczuk (Alismataceae) showed antagonistic effects against the contractions induced by angiotensin and bradykinin in rat ileum. However, they seem to be nonspecific antagonism.

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A Pharmacogenomic Study on Regional Dependent gene Expression and Drug Permeability in Rat Intestine

  • Shin, Ho-Chul;Chung, Moon-Koo;Han, Sang-Seop;Duxin Sun;Gordon L. Amidon
    • Proceedings of the Korean Society of Toxicology Conference
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    • pp.155-156
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    • 2003
  • RNA was isolated from mucosal tissue of the duodenum, jejunum, ileum and colon after perfusion. The gene expression profiles were measured using Affymetrix GeneChip(R) analysis. Prodrug valacyclovir permeability was 5-fold and 2-fold higher than the parent drug acyclovir in the jejunum and ileum, respectively.(omitted)

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Synthesis and Biological Activities of Carbamate Derivative (Carbamate 화합물의 합성 및 보건학적 연구)

  • 민경진
    • Journal of Environmental Health Sciences
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    • v.17 no.1
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    • pp.104-109
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    • 1991
  • Carbamates are generally used as insecticide, thus 8-hydroxy-5-chloroquinolinyl-N-ethylcarbamate was newly synthesized. Its physical properties were determined and chemical structure was identified by means of IR, nmr in addition to elemental analysis. The effect of the compound on rat's ileum, and antibacterial activity against Staphylococcus aureus, Salmonella typhi, E. coli, and Pseudomonas aeruginosa were examined. It was observed that the dosage over 100 $\mu$g/ml of the compound relaxed rat's ileum and the same dosage of the compound inhibited growth of the above strains of bacteria.

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The Screening of Biological Active Plants in Korea Using Isolated Organ Preparations (II) -Anticholinergic and Oxytocic Actions in the Ileum and Uterus- (적출장기표본(摘出臟器標本)에 의한 국산생약(國産生藥)의 생리활성(生理活性) 검색(檢索)(II) -회장(回腸) 또는 자궁(子宮)에서의 항(抗) Acetylcholine 및 Oxytocin작용(作用)-)

  • Woo, Won-Sick;Lee, Eun-Bang
    • Korean Journal of Pharmacognosy
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    • v.10 no.1
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    • pp.27-30
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    • 1979
  • The methanolic extracts of fifty medicinal plants were screened for anticholinergic and oxytocic activity in rat's ileum or uterus. In addition, their effect on the ileum and antagonism against oxytocin in the uterus were tested.

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Species Differences in Affinity and Efficacy of Carbachol for Ileal Muscarinic Receptors

  • Lee, Shin-Woong;Kim, Joo-Yeon
    • Proceedings of the Korean Society of Applied Pharmacology
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    • pp.87-87
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    • 1995
  • The muscarinic effects of carbachol were compared on the isolated ileums of guinea-pig, rat and rabbit to elucidate the underlying mechanism of species differences in sensitivity for carbachol. The ED$\_$50/ value estimated on the guinea-pig ileum was 4 to 6-fold lower than those obtained on the rat and rabbit ileums, but the K$\_$A/ values of carbachol determined by functional assays were almost identical with 12-l7 ${\mu}$M in all of three ileums. The competition data of carbachol for [$^3$H]QNB binding were best described by a two-site model yielding the Ki values of 0.4-0.6${\mu}$M and 12-16${\mu}$M for high(K$\_$H/) and low(K$\_$L/) affinity sites, respectively. The low affinity dissociation constants(K$\_$L/) of carbachol determined from receptor binding studies thus were not significantly different from the K$\_$A/ values estimated from functional studies. The percentage of receptor occupation that carbachol requires for half-maximal response was approximately 3 to 5-fold lower in guinea-pig compared to rat and rabbit whereas the density of muscarinic binding sites per gram of ileum measured by [$^3$H]QNB saturation isotherms was two-fold higher in guinea-pig than that in rat and rabbit. Therefore, the numbers of muscarinic receptors occupied at ED$\_$50/ values of carbachol were about two-fold lower in guinea-pig, suggesting two-fold greater intrinsic efficacy. These results indicate that the guinea-pig ileum has higher muscarinic receptor density and greater intrinsic efficacy for carbachol than the rat and rabbit ileums.

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The Screening of Biologically Active Plants in Korea Using Isolated Organ Preparation(V) -Anticholinergic and Oxytocic Actions in Rat's Ileum and Uterus- (적출장기표본(摘出臟器標本)에 의한 국산생약(國産生藥)의 생리활성(生理活性) 검색(檢索)(V) -흰쥐의 회장(回腸) 또는 자궁(子宮)에서의 항(抗) Acetylcholine 및 Oxytocin작용(作用)-)

  • Lee, Eun-Bang;Lee, Young-Soon
    • Korean Journal of Pharmacognosy
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    • v.22 no.4
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    • pp.246-248
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    • 1991
  • The methanolic extracts of forty-two medicinal plants were screened for direct effects on the isolated ileum and uterus and for anticholinergic and oxytocic effects on the respective organ preparation.

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Antihistamine Activities of Iminodiacetamide Derivatives

  • Rhee, Soo-Jin;Kam, Yoo-Lim;Seo, Young-Hee;ParkChoo, Hea-Young
    • Biomolecules & Therapeutics
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    • v.16 no.4
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    • pp.416-424
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    • 2008
  • A series of N,N'-substituted iminodiacetamide derivatives was synthesized and evaluated their inhibitory effects on the histamine-induced smooth muscle contraction in guinea-pig ileum and on the histamine release from IgE-sensitized RBL-2H3 cells (rat basophilic leukemia cell line). Compounds A3, A4 and A5 which have 1-(4-chlorobenzhydryl) piperazine moiety, showed both moderate antihistamine activity and histamine release inhibitory activity.