• Title/Summary/Keyword: Procaine

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Electrical Stimulation Causes Endothelium-Dependent Relaxation in Isolated Aortic Vessels of the Rabbit (토끼 흉부 대동맥 절편의 전기자극에 대한 수축 및 이완반응)

  • Lee, Seok-Gi;Choe, Hyeong-Ho;Lee, Jong-Un
    • Journal of Chest Surgery
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    • v.28 no.8
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    • pp.742-746
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    • 1995
  • The present study was aimed at investigating possible transmitter mechanisms in the endothelial cell layer in regulating the tone of the vascular smooth muscle. The thoracic aorta was isolated from the anesthetized male white rabbits and its helical strips were prepared. Electrical field stimulation was delivered to platinum wire electrodes positioned parallel to the vessel segment preconstricted with phenylephrine [3.5x10-6 mol/L at a distance of 1.5-2.0 mm. The electrical stimulation [70 V, 5 msec, 0.5-200 Hz caused either relaxation only [34% or a biphasic response [prolonged relaxation following a weak and transient contraction, 66% . The relaxation response was frequency- dependent, and at 200 Hz a complete relaxation was noted. Mechanical rubbing of the endothelial layer abolished or greatly attenuated the relaxation. The relaxation was also markedly attenuated in the presence of NG-nitro- L-arginine methyl ester [10-3mol/L or procaine hydrochloride [3.5x10-4mol/L . Tetrodotoxin,guanethidine, atropine or indomethacin failed to block or enhance the relaxation response to electrical field stimulation. It is concluded that the vascular endothelium in the aorta contains diffusible substances that regulates the function of the smooth muscle layer, in which relaxation is more prominent than contraction. Their release by the electrical stimualtion in vitro may not involve classic neuronal transmitter release mechanisms or metabolism of arachidonic acids by cyclooxygenase. The release of the relaxing agents may require an increase in cytosolic calcium level. The chemical nature of the relaxant may be, to a large extent, nitric oxide.

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The Action of Extract of Aconitum koreanum R. Raymond on Isolated Clam Heart (우리나라 백부자의 적출 조개 심장운동에 대한 작용)

  • Ha, Byoung-Kuk;Kim, Yoo-Sung;Kim, Won-Ja;Park, Chul-Hoon
    • The Korean Journal of Pharmacology
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    • v.8 no.1
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    • pp.15-25
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    • 1972
  • Korean aconitum (Aconitum koreanum R. Raymond) as one of the botanical crude drugs which pertain to helleboraceae has been extensively applied in Chinese medicine during the past decades. It has been particularly used in immortal tonic among the folk remedies in China, however, its general uses comprehend diuresis, cardiotonic, analgesia, neuralgia, gout and, furthermore, even neoplastic effect. The components of aconitum have been acknowledged as aconitine, mesaconitine, hypaconitine, aconine and so on. The main ingredient, aconitine has the advantage of causing the atrial fibrillation, but, its pharmacological research has not been fully elucidated. Although there are many reports with regard to the pharmacological effects on the motility of several animal hearts, their conclusions have not been regretfully coincided yet. The authors hereby paid attention to this point of view and made experiment to examine the relationship between the alcohol extract of Korean aconitum and the motility of the isolated clam heart, making the use of several drugs related to the heart such as serotonin, acetylcholine, pilocarpine, physostigmine, barium chloride, procaine and quinidine. The cardiac movement of the isolated clam (Meretrix lusoria) heart in the standard sea water solution was recorded with the electric kymograph according to the Magnus method. The results of the experiment are as follows. 1. The motility of the isolated clam heart represents the tendency of gradual inhibition in proportion to the concentration of AK-A $10^{-4}$, $5{\times}10^{-4}$, and $10^{-3}$. 2. The cardiac inhibitory effect of AK-A $10^{-3}$ antagonizes the motility of the isolated clam heart pretreated with serotonin $10^{-6}$. 3. The cardiac inhibitory effect of AK-A $10^{-3}$ antagonizes the systolic state appealed by barium chloride $10^{-3}$. 4. The systolic state caused by quinidine $10^{-4}$ is not inhibited by AK-A $10^{-3}$.

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Mechanism of the relaxant action of Trazodone in isolated rat aorta (흰쥐 대동맥에서 Trazodone의 혈관이완 작용기전)

  • Kim, Shang-jin;Kim, Jeong-gon;Kim, Jin-shang
    • Korean Journal of Veterinary Research
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    • v.43 no.4
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    • pp.587-595
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    • 2003
  • The aim of this study was to investigate trazodone's effect on vasorelaxation and blood pressure lowering and to examine its underlying mechanism of action in isolated thoracic aorta and anesthesized rats. Precontracted aortic rings with high KCl were relaxed with trazodone, at concentrations of $50{\mu}M$ or greater. However, precontracted rings with phenylephrine (PE) were relaxed with trazodone, at concentrations of $0.03{\mu}M$ or greater, in a concentration-dependent manner. These relaxant effects of trazodone on endothelium intact rat aortic rings were significantly greater than those on denuded rings. The trazodone-induced relaxations were suppressed by nitric oxide synthase (NOS) inhibitors, N(G)-nitro-L-arginine (L-NNA) and N(omega)-nitro-L-arginine methyl ester (L-NAME), guanylate cyclase inhibitors, methylene blue and 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ), a $Ca^{2+}$-activated $K^+$ channel blocker, tetrabutylammonium (TBA), a $Ca^{2+}$ channel blocker, nifedipine, $Na^+$ channel blockers, lidocaine and procaine, and removal of extracellular $Na^+$, but not by aminoguanidine, 2-nitro-4-carboxyphenyl-n, n-diphenylcarbamate (NCDC), indomethacin, glibenclamide and clotrimazole. In vivo, infusion of trazodone elicited significant decrease in arterial blood pressure. Trazodone-induced decrease in blood pressure was markedly inhibited by pretreatment of intravenous injection of saponin, L-NNA, methylene blue, TBA, lidocaine or nifedipine. These findings suggest that the endothelium-dependent relaxation and decrease in blood pressure induced by trazodone is mediated by release of NO from the endothelium, activation of TBA-sensitive $Ca^{2+}$-activated $K^+$ channels or inhibition of $Ca^{2+}$ entry through voltage-gated channel.

Effects of Local Anesthetics on the Rate of Rotational Mobility of Phospholipid Liposomes

  • Chung, In-Kyo;Kim, Dae-Gyeong;Chung, Yong-Za;Kim, Bong-Sun;Choi, Chang-Hwa;Cho, Goon-Jae;Jang, Hye-Ock;Yun, Il
    • BMB Reports
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    • v.33 no.3
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    • pp.279-284
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    • 2000
  • Using fluorescence probes, 2-(9-anthroyloxy) stearic acid (2- AS) and 12-(9-anthroyloxy) stearic acid (12-AS), we determined the differential effects of local anesthetics (tetracaine-HCI, bupivacaine-HCI, lidocaine-HCI, prilocaine-HCI and procaine-HCI) on the differential rotational rate between the surface (in carbon number 2 and its surroundings including the head group) and the hydrocarbon interior (in carbon number 12 and its surroundings) of the outer monolayer of the total phospholipid fraction liposome that is extracted from synaptosomal plasma membrane vesicles. The anisotropy (r) values for the hydrocarbon interior and the surface region of the liposome outer monolayer were$0.051{\pm}0.001$ and $0.096{\pm}0.001,$ respectively. This means that the rate of rotational mobility in the hydrocarbon interior is faster than that of the surface region. Local anesthetics in a dosedependent manner decreased the anisotropy of 12-AS in the hydrocarbon interior of the liposome outer monolayer, but increased the anisotropy of 2-AS in the surface region of the monolayer. These results indicate that local anesthetics have significant disordering effects on the hydrocarbon interior, but have significant ordering effects on the surface region of the liposome outer monolayer.

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Inhibitory effects of xylamine on the arterial contraction in rats (흰쥐 대동맥 수축에 대한 xylamine의 억제효과)

  • Kim, Sang-Jin;Kang, Hyung-sub;Kim, Jin-shang
    • Korean Journal of Veterinary Research
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    • v.44 no.3
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    • pp.389-397
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    • 2004
  • The therapeutic efficacy of xylamine in the field of psychological medicine has been recognized for years and the drug is used to treat depression and some other conditions, but little is known about its mechanism of action on vascular system. Therefore, the present study was designed to investigate the influence of xylamine on the contractile responses of isolated rat thoracic arteries to phenylephrine(PE) and potassium chloride(KCl). Xylamine produced a concentration-dependent relaxation in PE-precontracted endothelium intact(+E) rat aortic rings, but not in a KCl-precontracted aortic rings. Also, xylamine inhibited the PE-induced contraction in concentration-dependent manner, but not in the high KCl-induced contraction in +E rings. This concentration-dependent inhibition was suppressed by the removal of the endothelium (-E). The inhibitory effects of xylamine($0.3{\mu}M$) on the PE-induced contractions were suppressed by N(G)-nitro-L-arginine(L-NNA), N(omega)-nitro-L-arginine methyl ester(L-NAME), aminoguanidine, dexamethasone, methylene blue, 1H-[1,2,4]oxadiazolo [4,3-a]quinoxalin-1-one(ODQ), indomethacin, ryanodine, tetrabutylammonium(TBA), lidocaine, procaine and 0 mM extracellular $Na^+$, but not by 2-nitro-4-carboxyphenyl-n,n-diphenylcarbamate(NCDC), lithium, nifedipine, verapamil, 0 mM extracellular $Ca^{2+}$, glibenclamide and clotrimazole. These findings suggest that xylamine could act as a vasorelaxant and direct inhibitor of arterial contraction. This vasorelaxation involves an endothelial nitric oxide (NO)/cGMP (guanosine 3',5'-cyclic monophosphate) pathway or cyclooxygenase system, and an interference with $Ca^{2+}$ release, TBA-sensitive $Ca^{2+}$-activated $K^+$ channels and $Na^+$$ channels.

Resistance to local anesthesia in people with the Ehlers-Danlos Syndromes presenting for dental surgery

  • Schubart, Jane R.;Schaefer, Eric;Janicki, Piotr;Adhikary, Sanjib D.;Schilling, Amber;Hakim, Alan J.;Bascom, Rebecca;Francomano, Clair A.;Raj, Satish R.
    • Journal of Dental Anesthesia and Pain Medicine
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    • v.19 no.5
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    • pp.261-270
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    • 2019
  • Background: People with the Ehlers-Danlos Syndromes (EDS), a group of heritable disorders of connective tissue, often report experiencing dental procedure pain despite local anesthetic (LA) use. Clinicians have been uncertain how to interpret this apparent LA resistance, as comparison of EDS and non-EDS patient experience is limited to anecdotal evidence and small case series. The primary goal of this hypothesis-generating study was to investigate the recalled adequacy of pain prevention with LA administered during dental procedures in a large cohort of people with and without EDS. A secondary exploratory aim asked people with EDS to recall comparative LA experiences. Methods: We administered an online survey through various social media platforms to people with EDS and their friends without EDS, asking about past dental procedures, LA exposures, and the adequacy of procedure pain prevention. Among EDS respondents who both received LA and recalled the specific LA used, we compared agent-specific pain prevention for lidocaine, procaine, bupivacaine, mepivacaine, and articaine. Results: Among the 980 EDS respondents who had undergone a dental procedure LA, 88% (n = 860) recalled inadequate pain prevention. Among 249 non EDS respondents only 33% (n = 83) recalled inadequate pain prevention (P < 0.001 compared to EDS respondents). The agent with the highest EDS-respondent reported success rate was articaine (30%), followed by bupivacaine (25%), and mepivacaine (22%). Conclusions: EDS survey respondents reported nearly three times the rate of LA non-response compared to non-EDS respondents, suggesting that LAs were less effective in preventing their pain associated with routine office dental procedures.

Detection and Monitoring of Benzylpenicillin Residues in Livestock and Marine Products (유통 축·수산물 중 잔류벤질페니실린의 검출 및 모니터링)

  • Lee, Hyo Jeong;Kang, Young Won;Lee, Soo Min;An, Kyung A;Lee, Ryun Kyung;Seo, Sang Cheol;Lee, Ju Hee;Im, Moo Hyeog;Lee, Jeong Rim;Hong, Choong Man;Chang, Moon Ik;Cho, Yoon Jae
    • Korean Journal of Food Science and Technology
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    • v.46 no.3
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    • pp.288-294
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    • 2014
  • Penicillin and its salts, including the benzatine, procaine, and sodium salts, have been widely used in human and veterinary medicine. Owing to their low toxicity, they currently form the most important group of antibiotics. However, overdose and abuse of these antibiotics may lead to potential risk in human health. Therefore, this study was conducted to validate the analysis method established by the Korea Food Code in 2012 and to monitor the levels of benzylpenicillin residues in products with reference to the maximum residue level (MRL). Of the 232 product samples tested, benzylpenicillin was detected in 11 livestock products and 2 marine products. Benzylpenicillin concentrations were found to be lower than the MRL in 12 products; however, the concentration of benzylpenicillin was found to be greater than the MRL in 1 pork product. The limit of quantification (LOQ) for benzylpenicillin was found to be 0.001-0.002 mg/kg, with an average recovery of 90.4-115.3%. Calibrations showed good linearity of 0.995 over a range of 0.002-0.05 mg/kg.

THE EFFECTS OF THE PLATELET-DERIVED GROWTH FACTOR-BB ON THE PERIODONTAL TISSUE REGENERATION OF THE FURCATION INVOLVEMENT OF DOGS (혈소판유래성장인자-BB가 성견 치근이개부병변의 조직재생에 미치는 효과)

  • Cho, Moo-Hyun;Park, Kwang-Beom;Park, Joon-Bong
    • Journal of Periodontal and Implant Science
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    • v.23 no.3
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    • pp.535-563
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    • 1993
  • New techniques for regenerating the destructed periodontal tissue have been studied for many years. Current acceptable methods of promoting periodontal regeneration alre basis of removal of diseased soft tissue, root treatment, guided tissue regeneration, graft materials, biological mediators. Platelet-derived growth factor (PDGF) is one of polypeptide growth factor. PDGF have been reported as a biological mediator which regulate activities of wound healing progress including cell proliferation, migration, and metabolism. The purposes of this study is to evaluate the possibility of using the PDGF as a regeneration promoting agent for furcation involvement defect. Eight adult mongrel dogs were used in this experiment. The dogs were anesthetized with Pentobarbital Sodium (25-30 mg/kg of body weight, Tokyo chemical Co., Japan) and conventional periodontal prophylaxis were performed with ultrasonic scaler. With intrasulcular and crestal incision, mucoperiosteal flap was elevated. Following decortication with 1/2 high speed round bur, degree III furcation defect was made on mandibular second(P2) and fourth(P4) premolar. For the basic treatment of root surface, fully saturated citric acid was applied on the exposed root surface for 3 minutes. On the right P4 20ug of human recombinant PDGF-BB dissolved in acetic acid was applied with polypropylene autopipette. On the left P2 and right P2 PDGF-BB was applied after insertion of ${\beta}-Tricalcium$ phosphate(TCP) and collagen (Collatape) respectively. Left mandibular P4 was used as control. Systemic antibiotics (Penicillin-G benzathine and penicillin-G procaine, 1 ml per 10-25 1bs body weight) were administrated intramuscular for 2 weeks after surgery. Irrigation with 0.1% Chlorhexidine Gluconate around operated sites was performed during the whole experimental period except one day immediate after surgery. Soft diets were fed through the whole experiment period. After 2, 4, 8, 12 weeks, the animals were sacrificed by perfusion technique. Tissue block was excised including the tooth and prepared for light microscope with H-E staining. At 2 weeks after surgery, therer were rapid osteogenesis phenomenon on the defected area of the PDGF only treated group and early trabeculation pattern was made with new osteoid tissue produced by activated osteoblast. Bone formation was almost completed to the fornix of furcation by 8 weeks after surgery. New cementum fromation was observed from 2 weeks after surgery, and the thickness was increased until 8 weeks with typical Sharpey’s fibers reembedded into new bone and cementum. In both PDGF-BB with TCP group and PDGF-BB with Collagen group, regeneration process including new bone and new cementum formation and the group especially in the early weeks. It might be thought that the migration of actively proliferating cells was prohibited by the graft materials. In conclusion, platelet-derived growth factor can promote rapid osteogenesis during early stage of periodontal tissue regeneration.

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