• 제목/요약/키워드: Adrenergic receptor

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돼지 분만 시기의 조절에 관하여;IV. 자궁 평활근의 운동성에 대한 APT의 영향 (Control of Parturition Time on Pig;IV. Effect of ATP on Uterine Smooth Muscle Motility)

  • 박상은;황보원;변유성;조광제
    • 한국동물위생학회지
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    • 제19권2호
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    • pp.154-162
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    • 1996
  • The effcets of adenosine 5'-triphosphate(ATP) were investigated on the uterine smooth muscle motility in the pig. The results were summarized as follows: 1. The effects of the porcine uterine smooth muscle and the contractile responses increased between the concentration of ATP $10^{-5}$ and $10^{-3}$ M with a dose-dependent manner. 2. The contractile response induced by ATP($10^{-4}$ M) was not blocked by pretreatment with cholinergic receptor blocker, atropine ($10^{-6}$ M) 3. The contractile response induced by ATP ($10^{-4}$ M) was not blocked by pretreatment with $\alpha$ -adrenergic receptor blocker, phentolamine(10$^{-6}$ M) and ${\beta}$-adrenergic blocker, propranolol ($10^{-6}$ M). 4. The contractile response induced by ATP($10^{-4}$ M) was not appeared in 4Ca^{++}$ -free medium. As the concentration of $Ca^{++}$ in $Ca^{++}$ -free medium was increased, the contractile response induced by ATP ($10^{-4}$ M) was enhenced but was completely inhibited by pretreatment with $Ca^{++}$ -channel blocker, papaverine($10^{-6}$ M) or verapamil($10^{-6}$ M). From these results, it was conclued that the effects of ATP were the contraction mediated by purinergic receptor in uterine smooth muscle of pig.

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Haplotype Distribution of the β2-Adrenergic Receptor Gene in Korean Essential Hypertensives

  • Bae, Joon-Seol;Kang, Byung-Yong;Lee, Kang-Oh;Yoon, Tae-Joong;Kim, Jae-Hyoun;Kim, Ki-Tae
    • Toxicological Research
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    • 제18권3호
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    • pp.233-240
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    • 2002
  • In view of the effect of $\beta_2$-Adrenergic receptors ($\beta_2$-AR) as a risk factor for essential hypertension, we investigated the Fnu4HI and MnlI RFLPs of $\beta_2$ -AR gene in the Korean patients with essential hypertension and normal controls. There were no significant differences in the allele and genotype of these polymorphisms between normotensive and essential hypertensive subjects. In ethnic comparison, the allele frequencies of these three sites contained Nde I RFLP reported the association with essential hypertension in Korean population previously, were very different from those of other ethnic populations studied. The significant linkage disequilibrium was detected only in hypertensive group between Nde I and Fnu4HI sites. The Fnu4HI RFLP was also significantly associated with plasma triglyceride (TG) level. Therefore, our results suggest that the significant association between Fnu4HI variation in the human $\beta_2$-AR gene and plasma TG level may reflect the potential role of human $\beta_2$-AR gene as one of the genetic components for cardiovascular risk.

Cloning and expression of human $\beta$$_2$-adrenergic receptor in Saccharomyces cerevisiae

  • 장원진;안진현;고광호;강현삼
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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    • pp.295-295
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    • 1994
  • The human ${\beta}$$_2$-adrenergic receptor (h${\beta}$$_2$AR) contains seven clusters of hydrophobic amino acids suggestive of membrane-spanning domains and its gene is intronless. The genomic gene encoding h${\beta}$$_2$AR has been isolated by polymerase chain reaction. To express h${\beta}$$_2$AR in Saccharomyces cerevisiae, a modified h${\beta}$$_2$AR gene was fused to signal peptide sequence of Killer toxin gene from Kluyveromyces lactics. This fusion gene was expressed under the galactose-inducible GAL10 promoter. The ligand binding experiments showed that the functional h${\beta}$$_2$AR was expressed at a concentration three times as much as that found in Hamster lung.

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오수유가 선천성고혈압흰쥐의 혈압에 미치는 영향 (Effects Evodiae Fructus on the Blood Pressure in Spontaneously Hypertensive Rats)

  • 정수연;정수연;정수연;강주희;최기환;김주일
    • Biomolecules & Therapeutics
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    • 제8권4호
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    • pp.305-310
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    • 2000
  • The present study examined the effect of a methanol extract of Evodiae Fructus on the blood pressure in spontaneously hypertensive rats (SHR). The systolic blood pressure was measured after rats were pretreated with phentolamine, propranolol, or $N_{\omega}$-nitro-$_{L}$-arginine methyl ester(NAME) and subsequently received methanol extract of Evodiae Fructus. In SHR, intraperitoneal administration of methanol extract of Evodiae Fructus (0.5 mg/kg) produced antihypertensive effect that lasted for at least 4 hours. Antihypertensive effect of Evodiae Fructus was more stronger than that with $\alpha$-adrenergic receptor antagonist phentolamine and was not affected by $\beta$-adrenergic receptor antagonist propranolol. The antihypertensive effect of Evodiae Fructus was abolished by pretreatment of NAME. Our findings suggest Evodiae Fructus has an hypertensive effect, which may be mediated through nitric oxide synthesis.s.

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NOS만성억제로 인한 고혈압에서 아드레날린성 활성증가기전 (Mechanism of Increased Adrenergic Activities in Hypertension Induced by Chronic Inhibition of NOS)

  • 정국현;이석용
    • 약학회지
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    • 제45권1호
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    • pp.85-92
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    • 2001
  • Nitric oxide is a tonically produced vasodilator that maintains blood pressure in the normal animal. The chronic inhibition of nitric oxide synthase (NOS) elicits the hypertension in rats. However, the mechanism of hypertension induced by chronic inhibition of NOS is not clear. Thus, to clarify the mechanism of the occurance of hypertension, the changes in $\alpha$-adrenergic systems in rats treated with NOS inhibitors for 21 days were examined. Chronic administration of L-NAME significantly increased in the basal blood pressure, but chronic administration of 7-nitroindazole did not. Phenylephrine and G-protein stimulator elicited the more potent contraction in the aorta of the L-NAME-induced hypertensive rats. However when the contractile responses by phenylephrine and G-protein stimulator were calculated the proportion to the contraction by 25 mM KCL, there was no difference between the vehicle-treated rats and the L-NAME-treated rats. The density of $\alpha$-adrenergic receptors in aortic tissue was not changed by the chronic inhibition of NOS. These results suggest that hypertension induced by chronic inhibition of NOS is due to the inhibition of eNOS and the increased responses to the adrenergic drugs are due to the changes of the intracellular contactile mechanism of aortic tissue rather than the changes of receptor density.

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Higenamine이 토끼 페동맥에 미치는 영향 (Effect of Higenamine on Pulmonary Aorta of Rabbit)

  • 박찬웅;김봉기;최진석;임정규
    • 대한약리학회지
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    • 제28권1호
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    • pp.75-79
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    • 1992
  • Higenamine은 부자의 활성 성분의 하나로서 아드레나린성 beta-수용체를 통하여 강심효과를 나타내는 것으로 알려졌다. 본 연구는 norepinephrine 또는 potassium에 의한 토끼 페동맥의 수축에 미치는 Higenamine의 영향을 관찰한 것이다. 1. Norepinephrine으로 수축을 이르킨 폐동맥편은 higenamine의 전처치 또는 후처치로 용량의존적으로 이완되었다. 이같은 higenamine의 효과는 propranolol 전처치로 억제되었다. Higenamine의 propranolol에 대한 $pA_2$ 값은 8.25였다. 2. Higenamine의 페동맥편에 대한 효과는 phentolamine 전처치로 억제되지 않았다. 3. Isoproterenol도 norepinephrine에 의한 페동맥편 수축을 이완시켰으며 효력은 higenamine 보다 10배 켰다. 그러나 고농도$(3.3{\times}10^{-6})$의 isoproterenol은 내인성 활성을 보였다. 4. Higenamine과 isoproterenol은 potassium으로 유도된 페동맥편 수축에 대하여 이완효과를 나타내지 않았다. 이상의 결과로 미루어 higenamine은 혈관평활근에 대하여도 아드레나린성 beta-수용체를 통하여 이완효과를 나타낼 것으로 생각된다.

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자음건비탕 가지각ㆍ천마가 뇌허혈동물의 뇌혈유력학 변동 개선에 미치는 작용기전 (Mechanism of Jaeumgenby-tang adding Aurantii FructusㆍGastrodae Rhizoma on the Improvement against Changes of Cerebral Hemodynamics in Cerebral Ischemia Rats)

  • 정현우
    • 동의생리병리학회지
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    • 제17권5호
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    • pp.1194-1201
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    • 2003
  • Jaeumgenby-tang(JGT) have been used in oriental medicine for many centries as a therapeutic agent of vertigo caused by deficiency of qi(氣) and blood(血). Effect of Aurantii Fructus(AF) take off the phlegm by promoting the circulation of qi, Gastrodae Rhizoma(GR) has effects treating for headarch, vertigo by calming the liver and suppressing hyperactivity of the liver-yang (陽). I investigated whether injection of JGT adding AFㆍGR extract(JTG) affects cerebral hemodynamics [regional cerebral blood f1ow(rCBF), pial arterial diameter(PAD) in cerebral ischemia rats by MCA occlusion method, and I designed to make manifest whether JTG is mediated by adrenergic β-receptor, cyclooxygenase or guanylate cyclase. The changes of rCBF was determinated by laser-doppler flowmetry(LDF), and the changes of PAD was determinated by video microscope and width analyzer. The results were as follows in cerebral ischemic rats; The changes of rCBF and PAD were increased stabilizly by treatment with JTG(10 ㎎/kg, i.v.) during the period of cerebral reperfusion, and pretreatment with propranolol and indomethacin were increased JTG induced increase of rCBF and PAD during the period of cerebral reperfusion. Pretreatment methylene blue was decreased JTG induced increase of rCBF and PAD during the period of cerebral reperfusion. In conclusion, JTG causes a diverse response of rCBF and PAD, and action of JTG is mediated by adrenergic β-receptor and cyclooxygenase. I suggest that JTG has an anti-ischemic effect through the improvement of crebral hemodynamics.

Molecular Characterization and Expression Analysis of Adrenergic Receptor Beta 2 (ADRB2) Gene before and after Exercise in the Horse

  • Cho, Hyun-Woo;Shin, Sangsu;Song, Ki-Duk;Park, Jeong-Woong;Choi, Jae-Young;Lee, Hak-Kyo;Cho, Byung-Wook
    • Asian-Australasian Journal of Animal Sciences
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    • 제28권5호
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    • pp.686-690
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    • 2015
  • The adrenergic receptor beta 2 (ADRB2) plays a role in various physiological responses of the muscle to exercise, such as contraction and relaxation. Given its important role in muscle function, we investigated the structure of the horse ADRB2 gene and its expression pattern after exercise to determine if it can serve as a putative biomarker for recovery. Evolutionary analyses using synonymous and non-synonymous mutation ratios, were compared with other species (human, chimpanzee, mouse, rat, cow, pig, chicken, dog, and cat), and revealed the occurrence of positive selection in the horse ADRB2 gene. In addition, expression analyses by quantitative polymerase chain reaction exhibited ubiquitous distribution of horse ADRB2 in various tissues including lung, skeletal muscle, kidney, thyroid, appendix, colon, spinal cord and heart, with the highest expression observed in the lung. The expression of ADRB2 in skeletal muscle was significantly up-regulated about four folds 30 minutes post-exercise compared to pre-exercise. The expression level of ADRB2 in leukocytes, which could be collected with convenience compared with other tissues in horse, increased until 60 min after exercise but decreased afterward until 120 min, suggesting the ADRB2 expression levels in leukocytes could be a useful biomarker to check the early recovery status of horse after exercise. In conclusion, we identified horse ADRB2 gene and analyzed expression profiles in various tissues. Additionally, analysis of ADBR2 gene expression in leukocytes could be a useful biomarker useful for evaluation of early recovery status after exercise in racing horses.

자음건비탕가지각ㆍ천마가 뇌혈류역학 변동에 미치는 작용기전 (Mechanism of Jaeumgenby-tang adding Aurantii FructusㆍGastrodae Rhizoma on the Improvement and Changes of Cerebral Hemodynamics)

  • 임광모;박철훈;정현우
    • 동의생리병리학회지
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    • 제17권2호
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    • pp.416-422
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    • 2003
  • Jaeumgenby-tang(JGT) have been used in oriental medicine for many centuries as a therapeutic agent of vertigo caused by deficiency of qi(氣) and blood(血). Effect of Aurantii Fructus(AF) take off the phlegm by promoting the circulation of qi, Gastrodae Rhizoma(GR) has effects treating for headache, vertigo by calming the liver and suppressing hyperactivity of the liver-yang(陽). And, We reported that JGT adding AFㆍGR extract(JGTAG) was significantly increased regional cerebral blood f1ow(rCBF) by dilating pial arterial diameter(PAD). Therefor we designed to investigate whether JGTAG is mediated by adrenergic β-receptor, cyclooxygenase or guanylate cyclase in normal rats. The changes of rCBF and mean arterial blood pressure(MABP) were determinated by laser-doppler flowmetry(LDF), and the change of PAD was determinated by video microscope and width analyzer. The results were as follows in normal rats; Pretreatment with propranolol(1mg/kg, i.v.) was significantly inhibited JGTAG induced increase of rCBF, PAD and MABP, and pretreatment with indomethacin(1 mg/kg, i.v.) was significantly inhibited too. But pretreatment with methylene blue(10μg/kg, i.v.) were accelerated JGTAG induced increase of rCBF and MABP, but pretreatment with methylene blue was inhibited JGTAG induced increase of PAD. This results suggest that the mechanism of JGTAG is mediated by adrenergic β-receptor and cyclooxygenase.

Tumor Necrosis Factor ${\alpha}$ up-regulates the Expression of beta2 Adrenergic Receptor via NF-${\kappa}B$-dependent Pathway in Osteoblasts

  • Baek, Kyunghwa;Kang, Jiho;Hwang, Hyo Rin;Baek, Jeong-Hwa
    • International Journal of Oral Biology
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    • 제38권3호
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    • pp.121-126
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    • 2013
  • Tumor necrosis factor alpha ($TNF{\alpha}$) is a multifunctional inflammatory cytokine that regulates various cellular and biological processes. Increased levels of $TNF{\alpha}$ have been implicated in a number of human diseases including diabetes and arthritis. Sympathetic nervous system stimulation via the beta2-adrenergic receptor (${\beta}2AR$) in osteoblasts suppresses osteogenic activity. We previously reported that $TNF{\alpha}$ upregulates ${\beta}2AR$ expression in murine osteoblastic cells and that this modulation is associated with $TNF{\alpha}$ inhibition of osteoblast differentiation. In our present study, we explored whether $TNF{\alpha}$ induces ${\beta}2AR$ expression in human osteoblasts and then identified the downstream signaling pathway. Our results indicated that ${\beta}2AR$ expression was increased in Saos-2 and C2C12 cells by $TNF{\alpha}$ treatment, and that this increase was blocked by the inhibition of NF-${\kappa}B$ activation. Chromatin immunoprecipitation and luciferase reporter assay results indicated that NF-${\kappa}B$ directly binds to its cognate elements on the ${\beta}2AR$ promoter and thereby stimulates ${\beta}2AR$ expression. These findings suggest that the activation of $TNF{\alpha}$ signaling in osteoblastic cells leads to an upregulation of ${\beta}2AR$ and also that $TNF{\alpha}$ induces ${\beta}2AR$ expression in an NF-${\kappa}B$-dependent manner.