• Title/Summary/Keyword: acetylcholine

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Influence of Dichloroisoproterenol and Panax Ginseng on the action of some drugs. (Dichloroisoproterenol및 인삼(人蔘)의 이삼약물(二三藥物)의 작용(作用)에 미치는 영향(影響))

  • Chun, Yun-Sook;Choi, Baik-Hi;Kim, Chi-Euk;Lim, Kyu-Bok;Choi, Kyung-Hun
    • The Korean Journal of Pharmacology
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    • v.2 no.1 s.2
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    • pp.21-29
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    • 1966
  • Dichloroisoproterenol(DCI) i; one of the well known ${\beta}$-adrenergic receptor blocking agents. According to Moran and Perkins, DCI has sympathomimetic like action in relatively low concentrations. Fleming and Hawkins confirmed that DCI acts upon the receptors concerned with positive chronotropic and inotropic actions in the heart. Vogins reported that DCI, in concentration of $5{\times}10^{-8}$ to $5{\times}10^{-6}g/ml$, had properties of sympathomimetic amine causing positive inotropic and chronotropic actions in normal rat atria. And James and Nadeau found that DCI had not only adrenergic blocking effect in moderate and higher concentrations, but it also blocked the effect on the sinus node by vagal stimulation and of directly administered acetylcholine in higher concentrations. As stated above by many authors, DCI has complicated actions according to its concentrations. Our aim at the present experiments was to study the effects of DCI to the action of ouabain and acetylcholine upon the excised rabbit atria, as well as to the action of barium chloride and acetylcholine upon the excised rabbit intestine. In addition, Pan ax Ginseng is widely used as tonics in oriental nations, its pharmacological action, however, has not been clearly established. So we atempted to investigate the effects of the water extract of Panax Ginseng to the action of ouabain and DCI upon both atria and intestine. The results obtained were as follows. 1) DCI has a negative inotropic effect on the excised rabbit atria at concentration of $10^{-5}$ and a positive inotropic effect at concentration of $10^{-6}$. 2) DCI (at concentration of $10^{-6}$) potentiates the positive inotropic effect of ouabain upon the excised rabbit atria. 3) DCI antagonizes the action of acetylcholine upon the excised rabbit atria. 4) The water extract of Panax Ginseng, at concentration of $10^{-3}$, decreases the contractile force of rabbit atria, and tends to slightly increase that of rabbit atria at $10^{-4}$. 5) The water extract of Panax Ginseng exhibits a synergistic action with ouabain on the contractile force of rabbit atria. 6) DCI, in concentrations of $10^{-7}{\sim}10^{-6}$, depresses the tone and amplitude of contraction of the excised rabbit intestine. The depression of the intestinal tone markedly appears in pretreatment with reserpine 2mg/kg 24 hours. 7) DCI antagonizes the contractile effect of barium chloride on the excised rabbit atria. 8) DCI has no significant influence on the action of acetylcholine upon the excised rabbit intestine. 9) The series of those evidences indicates that DCI has a sympathomimetic-like action and more over a relaxing action directly on the excised rabbit intestine. 10) The water extract of Panax Ginseng in concentrations of $10^{-4}{\sim}10^{-3}$, has transient depression of the intestinal tone, but later gradually recovers its normal motility: 11) The water extract of Panax Ginseng has a synergistic action with ouabain on the intestinal contractility.

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Systemic Complications occurring after Korean Venomous Snake Bite, with focus on Hematologic and Neurologic Complications (독사 교상후 발생한 전신적 합병증 - 혈액학적 합병증과 신경학적 합병증을 중심으로 -)

  • Park, Eun-Jung;Yoon, Sang-Kyu;Ahn, Jung-Hwan;Choi, Sang-Cheon;Kim, Gi-Woon;Min, Young-Gi;Lee, Kuk-Jong;Jung, Ho-Sung;Jung, Yoon-Seok
    • Journal of The Korean Society of Clinical Toxicology
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    • v.7 no.2
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    • pp.90-96
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    • 2009
  • Purpose: This study explored and evaluated the systemic complications resulting from the bite of Korean venomous snake, focussing on hematologic and neurologic features. Methods: Medical records (demographic data, clinical measurements including laboratory results, severity score, and amount of antidote administration, and hospitalization course) of consecutive patients who presented with snakebites to two university teaching hospital during a 10-year period were retrospectively reviewed. Subgroup analysis was conducted for evaluations of anti-acetylcholine esterase administration in complicated victims. Results: The 170 patients displayed occurrence rates of hematologic and neurologic complications of 12.9% and 20.6%, respectively. Among 22 patients with hematologic complications, isolated thrombocytopenia was evident in eight patients (36.4%), prothrombin time (PT) / activated partial thromboplastin time (aPTT) prolongation in 11 patients (50.0%), and both in three patients (13.6%). The mean time to recovery was $4.5{\pm}1.8$ days for isolated thrombocytopenia, and $5.1{\pm}1.8$ days for PT and aPTT prolongation. Hematologic complications could occur suddenly 1?4 days after hospitalization. Among 35 patients with neurologic complications, dizziness was evident in 16 patients (45.7%), and diplopia / blurred vision in 19 patients (54.3%). The mean time to recovery was $3.4{\pm}0.6$ days in patients receiving anti-acetylcholine esterase and $6.9{\pm}1.8$ days in those not receiving anti-acetylcholine esterase (p=0.00). Conclusion: Occurrence rates of hematologic and neurologic complications following venomous snake bite differed as compared to other studies conducted in Korea. Onset of hematologic complications can occur rapidly days after admittance. Anti-acetylcholine esterase administration may be effective in treating neurologic complications.

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Screeening of Natural Plant Resources with Acetylcholine esterase inhibitory activity and Effect on Scopolamine-induced Memory Impairment (천연식물자원으로부터 Acetylcholine esterase 저해 활성 탐색 및 인지기능에 미치는 영향)

  • Choi, Jang Won;Won, Mu-Ho;Joo, Han-Seung
    • Journal of agriculture & life science
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    • v.45 no.6
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    • pp.213-226
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    • 2011
  • This study was performed to investigate the effect of essential oils and ethanolic extracts of approximately 650 plant species on acetylcholine esterase (AChE) enzyme activity using Ellman's colorimetric method in 96-well microplates. The results showed that the ethanolic extracts from twig of Sophora subprostrata, twig of Phellodendron amurense, seed of Corylopsis coreana, and essential oil (EO) from Citrus paradisi, Cupressus sempervirens, Ocimum basilicum, Pinus sylvestris and Rosmarinus officinalis inhibited more than 80% of AChE activity. Among these, EO from Pinus sylvestris, C. sempervirens and C paradisi exhibited higher values of AChE inhibitory activity, which were 75, 84 and 99% at a concentration of 50 ug/ml, respectively. Finally, EO from C paradisi (grapefruit, GEO) showed the highest inhibitory activity towards AChE, which showed 91% of inhibition at a concentration of 20 ug/ml. We also examined the anti-dementia effects of GEO in mouse by passive avoidance test and Morris water maze test. The model mouse (male, ICR) of dementia (negative control) was induced by administration of scopolamine (1 mg/kg body weight). The latency time of sample group administrated with GEO (100 mg/kg, p.o.) increased significantly as compared with negative control on passive avoidance test. There were significant recovery from the scopolamine-induced deficits on learning and memory in water maze test through daily administrations with GEO (100 mg/kg, p.o.). From these results, we conclude that GEO treatment might enhance the cognitive function, suggesting that the EO of C. paradis may be a potential candidate for improvement of perceptive ability and dementia.

Characterization of ion current induced by inhibitory and excitatory herbs in rat periaqueductal gray neuron (흰쥐 신경세포에서 억제성 및 흥분성 한약재가 유발한 이온전류의 특성)

  • Lee, Choong-Yeol;Cho, Sun-Hye;Seo, Jong-Eun;Han, Seung-Ho;Cho, Young-Wuk;Min, Byung-Il;Kim, Chang-Ju
    • The Journal of Korean Medicine
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    • v.19 no.2
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    • pp.450-467
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    • 1998
  • To research the characteristics of ion currents induced by inhibitory and excitatory herbs of oriental medicine, we used nystatin-perforated patch clamp technique under voltage clamp condition in periaqueductal gray neuron dissociated from Sprauge-Dawley rat, 10-15 days old. The results are as follows. 1. Ion current induced by $10mg/m{\ell}$ of Bupleuri Radix was inhibited $59.50{\pm}4.29%$ by $10^{-4}M$ bicuculline(p>0.01) but inhibition of $10.75{\pm}4.77%$ by $10^{-4}M$ tubocurarine and $4.75{\pm}4.23%$ by $10^{-4}M$ verapamil had no statistical significance(p>0.05). So ion current induced by Bupleuri Radix revealed only GABA induced $Cl^-$ current, not acetylcholine and $Ca^{2+}$ current. 2. Ion current induced by $20mg/m{\ell}$ of Coptidis Rhizoma was inhibited $47.20{\pm}7.88%$ by $10^{-4}M$ bicuculline(p<0.01) but $3.20{\pm}2.33%$ inhibition by $10^{-4}M$ tubocurarine and $1.00{\pm}1.00%$ inhibition by $10^{-4}M$ verapamil had no significance(p>0.05). So ion current induced by Coptidis Rhizoma revealed only GABA induced $Cl^-$ current, not acetylcholine and $Ca^{2+}$ current. 3. Ion current induced by $20mg/m{\ell}$ of Ecliptae Herba was inhibited $55.00{\pm}4.92%$ by $10^{-4}M$ bicuculline (p<0.01), and also inhibited $15.00{\pm}4.26%$ by $10^{-4}M$ tubocurarine(p<0.05), but inhibition of $6.00{\pm}3.03%$ by $10^{-4}M$ verapamil had no significance(p>0.05). So ion current induced by Ecliptae Herba showed GABA activated $Cl^-$ current and acetylcholine activated cation current, not $Ca^{2+}$ current 4. Ion current induced by $5mg/m{\ell}$ of Liriopis Tuber was inhibited $15.20{\pm}4.57%$ by $10^{-4}M$ bicuculline<0.05) and also inhibited $14.00{\pm}3.00%$ by $10^{-4}M$ tubocurarine(p<0.05), but inhibition of $5.20{\pm}4.80%$ by $10^{-4}M$ verapamil had no significance(p>0.05). So ion current induced by Liriopis Tuber showed GABA. activated $Cl^-$ current and acetylcholine activated cation current, not $Ca^{2+}$ current. 5. Ion current induced by $5mg/m{\ell}$ of Aconiti Tuber was inhibited $97.00{\pm}1.34%$ by $10^{-4}M$ bicuculline(p<0.01), $80.00{\pm}9.83%$ by $10^{-4}M$ tubocurarine(p<0.01), and $24.00{\pm}6.18%$ by $10^{-4}M$ verapamil(p<0.05). So ion current induced by Aconiti Tuber revealed GABA activated $Cl^-$ current and acetylcholine activated cation current and $Ca^{2+}$ current. 6. Ion current induced by $10mg/m{\ell}$ of Zingiberis Rhizoma was inhibited $33.00{\pm}7.43%$ by $10^{-4}$ bicuculline(p<0.05), $10.20{\pm}1.83%$ by $10-^{-4}M$ tubocurarine(p<0.01), and $14.00{\pm}2.16%$ by $10^{-4}M$ verapamil(p<0.01) So ion current induced by Zingiberis Rhizoma revealed GABA activated $Cl^-$ current and acetylcholine activated cation outtent and $Ca^{2+}$ current. 7. Ion current induced by $10mg/m{\ell}$ of Boshniakiae Herba was inhibited $65.00{\pm}13.75%$ by $10^{-4}M$ bicuculline(p<0.05), $38.00{\pm}9.24%$ by $10^{-4}M$ tubocurarine(p<0.05), and $33.25{\pm}7.42%$ by $10^{-4}M$ verapamiHp<0.05). So ion current induced by Bpshniakiae Herba revealed GABA activated $Cl^-$ current and acetylcholine activated cation current and $Ca^{2+}$ current. These results suggest that a point of difference between inhibitory and excitatory herbs is existence of$Ca^{2+}$ current.

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The Effect of ${\gamma}-Aminobutyric$ Acid on the Intestinal Motility of Rabbit (${\gamma}-Aminobutyric$ Acid가 토끼 장관운동에 미치는 영향)

  • Lee, Kae-Yurl;Lee, Myung-Hi;Jung, Hyung;Lim, Kyu-Parl
    • The Korean Journal of Physiology
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    • v.1 no.1
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    • pp.51-56
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    • 1967
  • In order to find out the effects of GABA on the rabbit's intestinal motility, the following experiments were carried out using Magnus method and the results obtained were as follows: 1. GABA inhibited the intestinal motility of rabbits initially. 2. GABA potentiated the inhibitory action of adrenaline and nor-adrenaline. 3. GABA inhibited the accelerating activity of acetylcholine on the intestinal motility by its anti acetylcholine effect. 4. The inhibitory action of GABA was unaffected with atropinization, strychnin, picrotoxin treatment, but the accelerating activity of GABA observed in some cases was only in the picrotoxin treatment.

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The Potentiating Effect of Sodium Nitroprusside on the Contraction Induced by Phenylephrino in Rat Aortic Rings (Phenylephrine에 의한 수축에 대한 Sodium Nitroprusside의 혈관수축 증대효과)

  • Je, Hyun-Dong
    • YAKHAK HOEJI
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    • v.50 no.3
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    • pp.208-213
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    • 2006
  • Rat aortic ring preparations were mounted in organ baths, exposed to sodium cyanide $(0.01{\sim}1.0\;mM)$ for 10 min, and then subjected to contractile agents or relaxants such as acetylcholine, sodium nitroprusside and isoproterenol. Presence of low concentration of sodium cyanide did not affect the contractile response to KCl or phenylephrine in the aortic rings with intact endothelium or endothelium denuded. Sodium nitroprusside but not acetylcholine or isoproterenol augmented phenylephrine-induced intact or denuded vascular contraction in the presence of low concentration of sodium cyanide. In conclusion, this study provides the evidence concerning the potentiating effect of sodium nitroprusside on the contraction induced by phenylephrine in rat aortic rings regardless of endothelial function.

Change of blood pressure end vasorelaxation on EAE-induced lewis rat

  • Bong su Kang;Park, Young shim;In hoi Huh
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1996.04a
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    • pp.194-194
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    • 1996
  • Pathogenesis of experimental allergic encephalomyelitis was involved with infection, inflammatory reaction, immune reaction etc. We studied on relation of blood vessel system and EAE. So, we measured blood pressure, heart rate and relaxation of isolated blood vessel in control and EAE-induced lewis rats. Blood pressure was decreased before EAE clinical sign (0-20day), but was increased from 23day. In isolated blood vessel, acetylcholine-treated relaxation was different on control, maximum EAE stage, recovery stage. Acetylcholine-treated relaxation was reduced 30% in recovery stage. but, sodium nitroprusside had similar relaxation reaction.

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Inhibition by Pinusolide of Platelet-Activating Factor (PAF-acether)-Induced Hypotension and Bronchoconstriction.

  • Kim, Kyung-A;Kim, Yeon-Su;Lee, Moo-Tak;Lee, Shin-Woong
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1996.04a
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    • pp.203-203
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    • 1996
  • It has been known that pinusolide isolated from Biota orientalis inhibits specifically [$^3$H] PAF binding to and PAF-induced aggregation of rabbit platelets in vitro. The present study was undertaken to evaluate the effects of pinusolide on hypotension and bronchoconstriction due to PAF. PAF(i.v.) in doses of 0.01 to 0.3 $\mu\textrm{g}$/kg induced a dose-dependent hypotension without tachyphylaxis in rat. Pinusolide(5~20 mg/kg, i.v.) inhibited PAF(0.03 $\mu\textrm{g}$/kg, i.v.)-induced hypotension dose-dependently, while it failed to block the hypotensive action of histamine, serotonin and acetylcholine. It inhibited bronchoconstriction and cutaneous vascular permeability induced by PAF in anesthetized guinea-pigs and rats, respectively, but it showed no inhibitory effect on the increase in bronchial resistance by histamine and acetylcholine. These results strongly suggest that in vivo pinusolide acts as a selective antagonist of PAF.

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