• YAKHAK HOEJI
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• v.47 no.2
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• pp.120-124
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• 2003

Due to its profound intestinal first-pass metabolism, oral eperisone hydrochloride produces a very low bioavailability and a very short muscle relaxant activity. To improve the efficacy and compliance of eperisone, we designed a new dosage form, the transdermal patch and evaluated the muscle relaxant effects of this patch in rats. The muscle relaxant activity was assessed by measurement of forelimb grip strength and hanging test in rats. The transdermal patch of eperisone hydrochloride showed significant muscle relaxant activity at 0.5, 1.5 and 3 cm$^2$/200 g rat (1.39, 4.17 and 8.33 mg of eperisone hydrochloride/kg, respectively) in a dose-dependent manner and the effects were lasted over 24 hours. The oral eperisone hydrochloride showed significant activity at 12.5, 25 and 50 mg/kg in a dose-dependent manner but the activity was within 1 or 2 hours after administration. These results suggest that the eperisone hydrochloride is absorbed efficiently from transdermal patch and the patch can exert potent and long-lasting muscle relaxant activity. This transdermal patch will increase the efficacy and compliance in the clinical use of eperisone hydrochloride.

• Archives of Pharmacal Research
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• v.27 no.12
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• pp.1194-1201
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• 2004

Michael addition of certain nucleophiles on ${\alpha}$ , ${\beta}$-unsaturated ketones 1 led to the formation of adducts 2-7 as well as the reaction of arylidene derivatives with secondary amines afforded the amino compounds 9 and 11. Also, dialkylmalonates were treated with ${\alpha}$-cyano cinnamide to afford 13. On the other hand, double Michael cycloaddition of ethylcyanoacetate or tetrachlorophthalic anhydride to the suitable divinylketone were synthesized to produce 15-17. Selected compounds (13 and 6) were screened for muscle relaxant, anticonvulsant, and sedative activities using established pharmacological models. Their activities were compared with that of phenobarbital sodium taken as standard. Compound 6 was the most potent muscle relaxant while compounds 13a and 13c offered the highest anticonvulsant activity. Meanwhile compound 13c showed the highest potentiation of phenobarbital induced sleep in mice.

• Archives of Pharmacal Research
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• v.12 no.3
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• pp.149-153
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• 1989

Seven 2, 3-diphenyl-5-methoxyindole derivatives were synthesized. The effect of structural variation of these molecules on biological activities was examined. None of the tested compounds was found to be toxic up 5 gm/Kg body weight. Four compounds demonstrated smooth muscle relaxant effects and one showed a persistent hypotensive effect. Only the parent compound, 2, 3-diphenyl-5-methoxyindole, showed a significant analgesic effect.

• Journal of Pharmacopuncture
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• v.25 no.3
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• pp.209-215
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• 2022

Objectives: Aqueous leaf extract of Tridax procumbens (ALETP) has potent relaxant activity. However, this relaxant activity in respiratory smooth muscle remains uninvestigated. This study investigates the effect of ALETP on the contractile activity of tracheal smooth muscle (TSM) in adult male Wistar rats. Methods: Twelve male Wistar rats divided into 2 groups and were treated with either 100 mg/kg of ALETP (ALETP treatment group) or vehicle (distilled water; control group) through oral gavage for 4 weeks. Dose responses of TSM from the 2 groups to acetylcholine (10^-9 to 10^-5 M), phenylephrine (10^-9 to 10^-5 M), and potassium chloride (KCl; 10^-9 to 10^-4 M) were determined cumulatively. Furthermore, cumulative dose responses to acetylcholine (10^-9 to 10^-5 M) after pre-incubation of TSM with atropine (10^-5 M), L-NAME (10^-4 M), indomethacin (10^-4 M), and nifedipine (10^-4 M), were determined. Results: Treatment with ALETP substantially inhibited TSM contraction stimulated by cumulative doses of acetylcholine, phenylephrine, and KCl. Furthermore, preincubation of TSM from the 2 groups in atropine significantly inhibited contractility in TSM. Incubation in L-NAME and indomethacin also significantly inhibited contractility in TSM of ALETP-treated rats compared to that of controls. Contractile activity of the TSM was also inhibited significantly with incubation in nifedipine in ALETP-treated rats. Conclusion: ALETP enhanced relaxant activity in rat TSM primarily by blocking the L-type calcium channel and promoting endothelial nitric oxide release. ALETP contains agents that may be useful in disorders of the respiratory tract.

• Journal of Pharmacopuncture
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• v.22 no.3
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• pp.122-130
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• 2019

Objectives: The medicinal plants are believed to enhance the natural resistance of the body to infections. Some of the main constituents of the plant and derived materials such as, proteins, lectins and polysaccharides have anti-inflammatory effects. Portulaca oleracea (P. oleracea) were used traditionally for dietary, food additive, spice and various medicinal purposes. This review article is focus on the anti-asthmatic effects of P. oleracea and its constituents. Methods: Various databases, such as the PubMed, Scopus, and Google Scholar, were searched the keywords including "Portulaca oleracea", "Quercetin", "Anti-inflammatory", "Antioxidant", "Cytokines", "Smooth muscle ", and " Relaxant effects " until the end of Jul 2018. Results: P. oleracea extracts and its constituents increased $IFN-{\gamma}$, IL-2, $IFN{\gamma}/IL-4$ and IL- 10/IL-4 ratio, but decreased secretion of $TNF-{\alpha}$, IL-4 and chemokines in both in vitro and in vivo studies. P. oleracea extracts and quercetin also signifcantly decreased production of NO, stimulated ${\beta}$-adrenoceptor and/or blocking muscarinic receptors in tracheal smooth muscles. Conclusion: P. oleracea extracts and quercetin showed relatively potent anti-asthmatic effects due to decreased production of NO, inflammatory cytokines and chemokines, reduced oxidant while enhanced antioxidant markers, and also showed potent relaxant effects on tracheal smooth muscles via stimulatory on ${\beta}$-adrenoceptor or/and blocking muscarinic receptors.

• Korean Journal of Veterinary Research
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• v.35 no.3
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• pp.459-469
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• 1995

As S-nitrosothiols were proposed as nitrergic carriers in vascular and nonvascular smooth muscle, we have investigated the relaxant properties of several S-nitrosothiols in the porcine retractor penis(PRP) muscle and compared them with the effects of exogenously added NO, electrical field stimulation(EFS) of NANC nerves and sodium nitroprusside(SNP). Also the influences of oxyhemoglobin and hydroquinone on the relaxant responses were investigated. In addition, effects of NO on membrane potentials and its involvement in the generation of inhibitory junction potential(IJP) were investigated with conventional intracellular microelectrode technique. The results were summerized as follows. 1. Frequency-dependent relaxations of PRP muscle were induced by EFS to NANC nerve. Tetrodotoxin($1{\times}10^{-6}M$) abolished the relaxations of PRP muscle induced by EFS, and L-NAME(($2{\times}10^{-5}M$) and methylene blue($4{\times}10^{-5}M$) inhibited the relaxations. L-NAME-induced inhibition of the relaxations was reversed by L-arginine($1{\times}10^{-3}M$), but not by D-arginine. 2. Exogenous NO($1{\times}10^{-5}-1{\times}10^{-4}M$), sodium nitroprusside(($1{\times}10^{-7}-1{\times}10^{-4}M$) induced dose-dependent relaxations of PRP muscle. All S-nitrosothiols($1{\times}10^{-7}-1{\times}10^{-4}M$) tested relaxed the PRP muscle in dose-dependent manner and the potency order was SNAP>GSNO>CysNO>SNAC. 3. Oxyhemoglobin($5{\times}10^{-5}M$) blocked the relaxation induced by exogenous NO and inhibited EFS-, S-nitrosothiols-, and SNP-induced relaxation. 4. Hydroquinone($1{\times}10^{-4}M$) also abolished the relaxations induced by exogenous NO, and reduced the relaxations induced by S-nitrosothiols, but did not affect EFS- and SNP-induced relaxations. 5. SNP($2{\times}10^{-6}-5{\times}10^{-6}M$) relaxed muscle strips but the membrane potentials were not affected. 6. EFS with several pulses(1ms, 2Hz, 80V) produced an inhibitory junction potential(IJP) with muscle relaxation. They were abolished by TTX($2{\times}10^{-6}M$). $N^G$-nitro-$_{\small{L}}$-arginine(L-NNA, $2{\times}10^{-5}M$) abolished the muscle relaxation, but had no effect on IJP.

• Natural Product Sciences
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• v.9 no.4
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• pp.260-263
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• 2003

Ethanol extract of the root of Clitoria ternatea Linn (CTEE) was evaluated for different neuropharmacological actions, such as general behaviour, exploratory behaviour, muscle relaxant activity and phenobarbitone induced sleeping time, in rats and mice. The extract was found to cause reduction in spontaneous activity, decrease in exploratory behavioural pattern by the head dip and Y- maze test, reduction in the muscle relaxant by rotarod, $30^{\circ}C$ inclined screen and traction tests. In addition CTEE significantly potentiated the phenobarbitone-induced sleeping time. Preliminary tests indicate that the ethanol extract of Clitoria ternatea Linn. At the doses of 100 and 150 mg/kg showed significant neuropharmacological activity.

• Archives of Pharmacal Research
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• v.29 no.1
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• pp.34-39
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• 2006

The antispasmodic and vasodilator activities of a newly synthesized piperidine derivative (1-(4'fluorophenacyl)-4-hydroxy-4-phenyl-piperidinium chloride) were studied in vitro. The test compound exhibited a dose-dependent relaxant effect on the spontaneous and $K^+$ (75 mM)-induced contractions of isolated rabbit jejunum with respective $EC_{50}$ values of 0.01 mM(0.01-0.02, 95% CI) and 0.30 mM (0.17-0.56). The $Ca^{++}$ channel blocking (CCB) activity was confirmed when the test compound (0.1-0.2 mM) shifted the $Ca^{++}$ dose-response curves to the right, similar to that produced by verapamil ($0.1-1.0{\mu}M$), a standard CCB. In the isolated rabbit aorta, the test compound showed a dose-dependent vasodilator effect on $K^+$ (75 mM)-induced contractions with an $EC_{50}$ value of 0.08 mM (0.02-0.26) while also suppressed the norepinephrine ($1{\mu}M$) control peak responses with $EC_{50}$ value of 0.08 mM (0.05-0.13, n=5). When tested in Langendorff perfused rabbit heart preparation, the test compound exhibited a negligible inhibitory effect on the rate or force of atrial and ventricular contractions when tested up to 5 mM. The results show smooth muscle-selective relaxant effect of the test compound on intestinal and vascular preparations mediated possibly via blockade of voltage and receptor-operated $Ca^{++}$ channels.

• Journal of Dental Anesthesia and Pain Medicine
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• v.22 no.2
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• pp.155-159
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• 2022

Cohen syndrome is a rare genetic disorder associated with mutations in the VPS13B gene. Individuals with this disorder present with diverse clinical manifestations, including muscle hypotonia, intellectual disabilities, and typical facial characteristics, such as prominent upper central incisors and micrognathia. General anesthesia was administered to a 23-year-old man with Cohen syndrome. Although we observed prominent upper central incisors, an overjet of 10 mm, micrognathia, and thyromental distance of 4 cm, hypotonia was not observed in the patient. Intubation was rendered difficult when performing a direct laryngoscopy. However, smooth intubation was achieved using a video laryngoscope. The patient's train of four (TOF) count remained zero close to 60 min after rocuronium administration, suggesting that the drug's muscle-relaxant effect may have been prolonged. A TOF ratio of 0.79 was confirmed 130 min after rocuronium administration, and a TOF ratio of 1.0 was confirmed after administration of 150 mg of sugammadex. The patient's respiration remained stable after extubation, and no recurarization of muscle relaxation was observed. As demonstrated in this case report, it is important to closely monitor recovery from muscle relaxation and prepare multiple techniques for airway management in general anesthesia management of patients with Cohen syndrome.

• Advances in Traditional Medicine
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• v.6 no.3
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• pp.221-231
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• 2006

The aim of the present study is to investigate central nervous system (CNS) activity of the methanol extracts of leaves of Caesalpinia bonducella (MECB) and stem bark of Bauhinia racemosa (MEBR) (Caesalpinaceae) in Swiss albino mice and Wistar albino rats. General behavior, exploratory behavior, muscle relaxant activity and phenobarbitone sodium-induced sleeping time were studied. The results revealed that the methanol extracts of leaves of Caesalpinia bonducella at 100 - 200 mg/kg and stem bark of Bauhinia racemosa 100 - 200 mg/kg caused a significant reduction in the spontaneous activity (general behavioral profile), remarkable decrease in exploratory behavioral pattern (Y-maze and head dip test), a reduction in muscle relaxant activity (rotarod and traction tests), and also significantly potentiated phenobarbitone sodium-induced sleeping time. The results suggest that MECB and MEBR exhibit CNS depressant activity in tested animal models.