• Korean Journal of Veterinary Research
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• v.37 no.2
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• pp.331-338
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• 1997

최근 동물의 진통 및 진정을 목적으로 널리 사용되고 있는 imidazole 유도체인 clonidine, medetomidine, etomidate 등의 약물과 xylazine의 효과를 발정정지기의 척출 돼지 자궁근에서 검토하였다. Clonidine($10^{-8}{\sim}10^{-6}M$)이나 medetomidine($10^{-8}{\sim}10^{-6}M$)은 xylazine과 비슷한 정도로 용량의존적인 자궁근의 수축을 일으켰다. Clonidine, medetomidine, xylazine 등의 $EC_{50}$는 각각 24.7nM, 19.9nM, 45.1nM이었다. 그러나 etomidate는 $10^{-6}M$ 미만의 농도에서 반응이 거의 없었으며, $10^{-6}M$ 이상에서 수축반응을 일으켰다. 이들 agonists의 효과는 yohimbine($10^{-8}{\sim}10^{-6}M$), idazoxan($10^{-7}{\sim}10^{-5}M$), tolazoline($10^{-7}{\sim}10^{-5}M$) 등의 ${\alpha}_2-adrenoceptor$ antagonists에 의해서 차단되었으나, ${\alpha}_1-adrenoceptor$ antagonist인 prazosin ($10^{-6}M$)에 의해서는 차단되지 않았다. 또한 $Ca^{2+}-free$ medium이나 verapamil($10^{-5}M$)의 전처치에 의해서 이들 agonist의 효과가 완전히 차단되었다. 결론적으로 발정정지기의 돼지 자궁근에서 clonidine, medetomidine, etomidate, xylazine 등은 ${\alpha}_2-adrenoceptors$의 흥분을 통해 자궁근의 수축을 일으키며, 이 효과는 voltage-dependent $Ca^{2+}$ channels을 통한 extracellular $Ca^{2+}$ influx의 증가에 의한 것으로 추론하였다.

• Bulletin of the Korean Chemical Society
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• v.31 no.2
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• pp.447-452
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• 2010

A series of 5-alkoxy-tetrazolo[1,5-a]quinolines were synthesized to evaluate their anticonvulsant and antidepressant effects. Anticonvulsant effects and neurotoxicity of the compounds when injected intraperitoneally to mice were determined by a maximal electroshock (MES) test and a rotarod test, respectively. Only three of the synthesized compounds (4a, 4b, 4c) displayed anticonvulsant activity at a dose of 300 mg/kg. Most of the compounds significantly reduced immobility times during the forced swimming test (FST) at a dose of 100 mg/kg, indicative of antidepressant activity. Among the compounds, 5-(2-fluorobenzyloxy)tetrazolo[1,5-a]quinoline (4k) reduced immobility time by 66.85% at 30 mg/kg compared with the same dose of Fluoxetine, which reduced immobility time by 52.30%. According to the results of the 5-Hydroxytryptophan induced head-twitch test and yohimbine toxicity potentiation test, the noradrenergic system seems not to be involved in the antidepressant-like effect of compound 4k while the serotonergic system seems a little to be involved.

• Korean Journal of Veterinary Research
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• v.32 no.3
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• pp.341-345
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• 1992

The tuber of Pinellia ternata Breitenbach(Araceae), which is distributed in Korea, China, and Japan, has been used in traditional Chinese medicine. The prescription containing Pinellia tuber shows anti-emetic, sedative, and anti-tussive effects. The purpose of this study was to investigate the effects of Pinellia ternata tuber on the xylazine-induced emetic and sedative responses in cats. The results were as follows ; 1. Intramuscular injection of xylazine hydrochloride(1.0mg/kg) reliably evoked vomiting with an incidence of 100% and sedated with a mean sedation time of 34.22 min. 2. The xylazine-induced emetic and sedative responses were not prevented by oral administration of powder (0.5g/head), decoction ($1.0m{\ell}/100g$), and methanol extract ($0.1m{\ell}/100g$) of the Pinellia ternata tuber. 3. The xylazine-induced emetic and sedative responses were inhibited by intravenous injection of decoction($0.3m{\ell}/100g$) of the Pinellia ternata tuber. 4. The xylazine-induced emetic and sedative responses were inhibited by intravenous injection of a combined mixture of yohimbine hydrochloride(0.125mg/kg) and 4-aminopyride(0.3mg/kg).

• Korean Journal of Veterinary Research
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• v.34 no.3
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• pp.479-486
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• 1994

Effects of catecholamines and the site of receptor of catecholamines were investigated in the longitudinal muscle of the rumen. In order to this experiment, specimens were obtained from 35 Korean Native Cattles, 2-3 years old, in the Kwang-ju area slaughterhouse. Longitudinal muscle strips of rumen were made from sample, and then measured the isometric contraction with physiograph in $37{^{\circ}C}$ organ bath. The results were summarized as follows. 1. 30% of all strips showed rhythmic contraction after short incubation time. 2. Relaxation produced by catecholamines in this preparations increased in a dose-dependant manner. 3. Isoproterenol(${\beta}$-agonist) caused relaxation, but phenylephrine(${\alpha}_1$-agonist) and xylazine(${\alpha}_2$-agonist) were unaffected. 4. The relaxation induced by epinephrine and norepinephrine were not affected by phentolamine(${\alpha}$-blocker) and prazosin(${\alpha}_1$-blocker), yohimbine(${\alpha}_2$-blocker). But propranolol(${\beta}$-antagonist) abolished the effect of catecholamines on relaxation. 5. It is concluded that catecholamines produced relaxation in the longitudinal muscle of rumen via the ${\beta}$-adrenoceptor.

• Journal of Chest Surgery
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• v.23 no.6
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• pp.1107-1117
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• 1990

The regulatory role of the post \ulcorner1-and \ulcorner2-adrenoceptors on cardiac function, particularly in coronary flow rate, was investigated in the isolated rat heart treated with 10-6 M propranolol. When introduced into the left atrium of the heart, phenylephrine[10-7-10-2 M] decreased coronary flow rate and increased mean coronary resistance in a dose related fashion, but did not affect heart rate. Methoxamine also elicited the increment of coronary resistance and the decrement of coronary flow rate, though the effects of methoxamine were weaker than those by phenylephrine. The effect of phenylephrine was inhibited by 1\ulcornerM prazosin and shifting the dose-response curve to the right. The effects of clonidine, a selective \ulcorner2-adrenoceptor agonist, were studied in the heart taken from reserpinized rats. Clonidine increased coronary resistance, decreased heart rate and coronary flow rate with a dose-dependent manner. These effects were abolished by 10-6 M yohimbine, a selective \ulcorner2-antagonist, and were not affected by 10-6M prazosin. Clonidine also decreased coronary flow and increased mean coronary resistance in electric paced heart. These effects were inhibited by rawoulscine, a selective ca-antagonist. These results indicate that the stimulation of both post \ulcorner1-and \ulcorner2-adrenoceptor causes coronary vasoconstiction. And it is inferred that this model of sympathomimetics-induced coronary vasospasm may provide a useful tool for investigating spasmolytic agents which are of benefit in the treatment of variant angina.

• Korean Journal of Plant Resources
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• v.23 no.6
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• pp.513-518
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• 2010

In the present study, the antinociceptive profiles of Dianthus chinensis L extract were examined in ICR mice. Dianthus chinensis L extract administered orally (200 mg/kg) showed an antinociceptive effect as measured by the tail-flick and hot-plate tests. In addition, Dianthus chinensis L extract attenuated the writhing numbers in the acetic acid-induced writhing test. Furthermore, the cumulative nociceptive response time for intrathecal (i.t.) injection of substance P ($0.7\;{\mu}g$) was diminished by Dianthus chinensis L extract. Intraperitoneal (i.p.) pretreatment with yohimbine ($\alpha_2$-adrenergic receptor antagonist) attenuated antinociceptive effect induced by Dianthus chinensis L extract in the writhing test. However, naloxone (opioid receptor antagonist) or methysergide (5-HT serotonergic receptor antagonist) did not affect antinociception induced by Dianthus chinensis L extract in the writhing test. Our results suggest that Dianthus chinensis L extract shows an antinociceptive property in various pain models. Furthermore, this antinociceptive effect of Dianthus chinensis L extract may be mediated by $\alpha_2$-adrenergic receptor, but not opioidergic and serotonergic receptors.

• Archives of Pharmacal Research
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• v.12 no.4
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• pp.243-248
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• 1989

Effects of B-HT 920 on the vagally stimulated gastric acid secretion were studied in anesthetized and gastric fistula rats. When the gastric acid secretion was increased by stimulation of the vagus nerve, B-HT 920 was partially attenuated by prazosin, $\alpha_1-$adrenoceptor antagonist and virtually abolished by yohimbine, $\alpha_2-$adrenoceptor antagonist. On the other hand, when the gastric acid secretion was increased by the infusion of bethanechol, a muscarinic parasympathetic stimulant, B-HT 920 had no effect on the bethanechol-induced gastric acid secretion. These results suggest that B-HT 920 inhibits vagally induced gastric acid secretion by activation of presynaptic $\alpha-$adrenoceptors located on the vagally stimulated pathways in the gastric wall and this effect of B-HT 920 is more related to $\alpha_2-$adrenoceptors than $\alpha_1-$adrenoceptors.

• Korean Journal of Veterinary Research
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• v.35 no.2
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• pp.255-261
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• 1995

Amitraz frequently causes the side effect of intestinal stasis or bloat in mammals. It is very similar to the side effect of xylazine or clonidine which produce the inhibition of intestinal motility through the stimulation of ${\alpha}_2$ adrenoceptor. Therefore, we examined whether amitraz causes intestinal stasis or bloat through the inhibition of intestinal motility or whether amitraz produces the inhibition of intestinal motility through the stimulation of ${\alpha}_2$ adrenopceptor. Amitraz inhibited the intestinal motility in a dose-dependent manner in isolated rabbit jejunum and isolated pig ileum. These inhibitory effects of amitraz were blocked by yohimbine but not by prazosin. The effect of intestinal contraction of carbachol or high-potassium was not affected by the pretreatment of amitraz. However, the con-traction of histamine was inhibited by the pretreatment of amitraz. It is concluded that amitraz mainly inhibits the intestinal motility through the stimulation of ${\alpha}_2$-adrenoceptor although partially antihistaminic action of amitraz can be involved.

• Korean Journal of Veterinary Research
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• v.39 no.4
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• pp.710-714
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• 1999

In veterinary medicine amitraz has been used as an insecticide to eliminate mites, lice, and ticks in dogs, cats, goats, swine and cattle. We performed the experiment on bradycardiac effect of arnitraz in rabbits. Under anesthetized with urethane (1g/kg, 25% w/v, SC), the femoral artery was cannulated by a polyvinyl tube which was connected with pressure transducer for continuous measurement of heart rate. Amitraz (0.5-2.5mg/kg, IV) reduced the heart rate in a dose-dependent manner. Pretreatment of yohimbine (2.0mg/kg) or atropine (2.0mg/kg and 4.0mg/kg) affected the response of amitraz but pretreatment of prazosin (0.5mg/kg) or propranolol (1.0mg/kg) did not. Moreover, the effect of amitraz was blocked by vagotomy. The result of our experiment suggest that amitraz may reduce the heart rate by increasing acetylcholine through activating vagal nerves and ${\alpha}_2$-adrenoceptors could be involved in activating vagal nerves.

• The Korean Journal of Physiology
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• v.22 no.1
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• pp.89-100
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• 1988

Effect of clonidine on the dorsal horn cell responses to mechanical stimulations were studies in 3 spinalized cats and 10 cats with intact spinal cord. The type of dorsal horn cells was determined according to their response patterns to four graded mechanical stimulations (brush, pressure, pinch and squeeze) applied to the respective receptive fields. In the present study the results obtained only from the wide dynamic range (WDR) cells were included. The responses of the WDR cells to noxious mechanical stimuli were selectively suppressed following intravenous administration of clonidine into the experimental animals. The clonidine-induced changes in responses of the WDR cells to mechanical stimulation were not affected by naloxone or propranolol whereas effect of clonidine on WDR cell responses was almost completely abolished after intravenous administration of yohimbine. Also in the spinalized cats results parallel to those observed in cats with intact spinal cord were obtained. The results of present study strongly implies that analgesic action of clonidine can be mediated through excitation of ${\alpha}_{2}-adrenoceptor$ even at the spinal cord level without supraspinal mechanism.