• Title/Summary/Keyword: Beta-adrenergic receptor

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The Studies on Glycogenolytic Adrenergic Receptor in Rat (흰쥐에서의 해당작용(解糖作用) Adrenergic Receptor에 대(對)한 검토(檢討))

  • Park, C.W.;Cha, I.J.
    • The Korean Journal of Pharmacology
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    • v.16 no.1 s.26
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    • pp.9-14
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    • 1980
  • To evaluate the adrenergic receptors for glycogenolytic responses to catecholamine, the blood glucose level, liver glycogen content and muscle glycogen level in rats were studied with treatment of epinephrine, norepinephrine and isoproterenol. In addition, to study the possibility of interconversion of adrenergic receptors, the effects of catecholamines in feeding animal were compared with those in fasting animal. The results are summarized as follow; 1) Epinephrine and norepinephine showed dose dependent increase of blood glucose level but the effect of isproterenol was not significant. 2) The prandial states of animal did not influence on effects of catecholamines on blood glucose level. 3) Liver glycogen contents were lowered by epinephrine or by norepinephrins but effect of isoproterenol was not significant. 4) Glycogen content of skeletal muscle was significantly lowered by isoproterenol and. epinephrine shifted the dose-response curve to right, but the effect of norepinephrine was not significant. 5) The effects of epinephrine and norepinephrine on blood glucose were significantly blocked by ergotamine but not by propranolol. These results indicate that the glycogenolytic response to adrenergic agents in rat is mediated by an alpha-receptor in liver and by a beta-receptor in skeletal muscle.

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Mutation Analysis in β2-Adrenergic Receptor Gene by Single Strand Conformation Polymorphism (SSCP) and Denaturing High Performance Liquid Chromatography (DHPLC) (SSCP와 DHPLC에 의한 β2-교감신경수용체 유전자의 돌연변이 분석)

  • Park, Sang-Bum;Han, Sang-Man;Nam, Youn-Hyoung;Jang, Won-Cheoul
    • Analytical Science and Technology
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    • v.17 no.1
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    • pp.53-59
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    • 2004
  • Up to now, methods for the detection of genetic alterations as single strand conformation polymorphism (SSCP) or denaturing gradient gel electrophoresis (DGGE) have been used. It is too labor-intensive and expensive to serve for routine analysis. Moreover, lower in its sensitivity and specificity being also strongly dependent on the experience of the investigater. To improve these problems, we analysed mutation of ${\beta}_2$-adrenergic receptor gene that controls bronchial asthma by denaturing high performance liquid chromatography (DHPLC) according to ion-pair reversed phase chromatography (IP-RPC). We extracted genomic DNA from 80 asthma patients and then amplified DNA using PCR and analysed PCR product by SSCP and DHPLC. As a result, we analysed mutation frequency is 19 (23.75%) on SSCP and 25 (31.25%) on DHPLC in ${\beta}_2$-adrenergic receptor gene. We conclude that DHPLC is a fast and simple screening method rather than SSCP analysis.

Studies on the Physiological Properties of the Histamine Receptor of Ileal Smooth Muscle in Dog (개 회장 평활근에 있어서 Histamine Receptor의 생리적 특성에 관한 연구)

  • Kim, Joo-heon;Park, Yong-bae;Kwun, Jong-kuk
    • Korean Journal of Veterinary Research
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    • v.24 no.1
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    • pp.17-23
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    • 1984
  • To validate the physiological properties of the histamine receptors of ileal smooth muscle in dog, the effects of adrenergic-, cholineric-, and H-receptor antagonists on the responses of ileal smooth muscle strips to histamine were investigated. The results were summarized as follows; 1. Histamine caused the contraction of ileal smooth muscle and the contractile responses were increased between the concentration of histamine $10^{-7}M$ and $10^{-5}M$ with dose-dependent manner in dog. 2. The shorter the treatment interval of histamine, the lower the contractile activity until the treatment interval extended to 40 minutes. 3. The contractile response induced by histamine was completely blocked by the pre treatment with a $H_1$-receptor blocker, chlorpheniramine and not by the pretreatment with a $H_2$-receptor blockers cimetidine. 4. The contractile response induced by histamine was not blocked by the pretreatment with a cholinergic receptor blocker, atropine. 5. The contractile response induced by histamine was not blocked by the pretreatment with an ${\alpha}$-adrenergic receptor blocker, phenoxybenzamine, or a ${\beta}$-adrenergic receptor blocker, propranolol. From these results, it was suggested that the contraction induced by histamine was elicited through $H_1$-receptor on the ileal smooth muscle in dog.

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Localization of adrenergic receptors in bovine esophageal groove (소(牛) 식도구 평활근의 Adrenergic receptor 존재부위에 관한 연구)

  • Kang, Tong-mook;Cho, Je-yoel;Park, Jun-hong;Yang, Il-suk
    • Korean Journal of Veterinary Research
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    • v.33 no.4
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    • pp.617-622
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    • 1993
  • The preliminary studies on the localization of adrenoceptors were performed on smooth muscle strips of bovine esophageal groove. The mechanical activity of the muscle strip was recorded isometrically in vitro.w In the bottom circular muscle strips. the excitatory ${\alpha}-adrenergic$ responses were not blocked by tetrodotoxin$(2.1{\times}10^{-6}M)$ and denervation which was carried by cold storage of strips for 48 hrs in Tyrode's solution at $5-6{^{\circ}C}$ without oxygen supply. These excitatory ${\alpha}-adrenergic$ responses were partially blocked by atropine. In the lip longitudinal muscle strips, the inhibitory${\beta}-adrenergic$ responses were not blocked by pretreatment of tetrodotoxin and atropine. The results suggest that ${\beta}-adrenergic$ receptors mediating relaxations are located on the postsynaptic smooth muscle cells, whereas ${\beta}-adrenergic$ receptors mediating contractions are located both in the smooth muscle cells and in the cholinergic neurones.

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Effect of transmural stimulation to motility on isolated gastric smooth muscle (토끼 적출 위 평활근의 운동성에 대한 transmural stimulation의 효과)

  • Kim, Joo-heon;Shim, Cheol-soo;Hong, Yong-geun
    • Korean Journal of Veterinary Research
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    • v.39 no.3
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    • pp.472-477
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    • 1999
  • To elucidate the action of the cholinergic and adrenergic nerve on isolated gastric fundus smooth muscle of rabbit, the effects of electrical transmural stimulation were investigated in the presence of atropine, cholinergic receptor blocker; phentolamine, nonselective ${\alpha}$-adrenergic receptor blocker; propranolol, nonselective ${\beta}$-adrenergic receptor blocker and L-arginine from the isometric contraction of physiological recording system. 1. The contractile response induced by electrical transmural stimulation was increased as the frequency(1~32Hz)-dependent manner on the isolated gastric fundus smooth muscle. 2. The contractile response induced by electrical transmural stimulation was markedly inhibited by the pretreatment of atropine($1{\mu}M$). 3. The contractile response induecd by electrical transmutal stimulation was inhibited by the pretreatment of phentolamine($1{\mu}M$). 4. The relaxative response induced by electrical transmural stimulation on presence of atropine ($1{\mu}M$) was inhibited by the pretreatment of propranolol($1{\mu}M$). 5. The relaxative responses on precontraction induced by histamine($10{\mu}M$) with guanethidine ($50{\mu}M$) and atropine($1{\mu}M$) by electrical transmural stimulation were increased by L-arginine (1mM). These findings suggest that it was the excitatory action of cholinergic and ${\alpha}$-adrenergic nerve, and the inhibitory action of ${\beta}$-adrenergic nerve and nonadrenergic noncholinergic nerve on the isolated gastric fundus smooth muscle of rabbit.

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Effect of Calcium Antagonists on the Cardiac ${\beta}$-Adrenergic Receptors (칼슘 길항제가 심장 ${\beta}$-Adrenergic Receptors에 미치는 영향)

  • 이신웅;김정구
    • Biomolecules & Therapeutics
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    • v.1 no.1
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    • pp.1-8
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    • 1993
  • It has been known that calcium antagonists also inhibit the radioligand binding to muscarinic and $\alpha$-adrenergic receptors and, in case of verapamil, these inhibitions may play a role in the effects of verapamil on the heart. In this study, the effects of nicardipine, nifedipine, nimodipine, diltiazem and verapamil on the binding of [$^3H$]dihydroalprenolol (DHA) to dog cardiac ${\beta}$-adrenergic receptors were examined. A single uniform [$^3H$]DHA binding site ($K_D/= 5nM\;and\;B_{max}=2600$ fmol/mg protein) was identified in dog cardiac sarcolemma. [$^3H$]DHA binding was not affected by the usual therapeutic concentrations of these calcium antagonists (nanomolar range) but in the "nonspecific"concentration ranges ($28-180{\mu}m$) these drugs inhibited [$^3H$]DHA binding to $\beta$-adrenergic receptors. Nicardipine, nifedipine, nimodipine and diltiazem competed for [$^3H$]DHA binding to ${\beta}$-adrenergic receptors with dissociation constants ($K_i$) of $28{\mu}m,\' 74{\mu}m, 39{\mu}m \;and \;35{\mu}m,$ respectively. Verapamil ($K_i=176.5 {\mu}m$) was less potent inhibitor than other drugs and this inhibition was noncompetitive; the maximal binding capacity ($B_{max}$) $300 {\mu}m$ verapamil without change in the apparent dissociation constant (4K_D$) for DHA. These results indicate that the inhibitory action of calcium antagonists at high concentrations on ${\beta}$-adrenergic receptors is not involved in the therapeutic effects of these drugs by the calcium channel blocking action.

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Pharmacological characteristics of higenamine on adrenergic β-receptors (아드레날린성 β-수용체에 대한 higemamine의 약리학적 특성)

  • Yun, Hyo-in;Chang, Ki-churl;Lee, Chang-eop
    • Korean Journal of Veterinary Research
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    • v.32 no.1
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    • pp.41-49
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    • 1992
  • Higenamine is an Aconiti tuber derived compound whose chemical structure is 1-(4'-hydroxybenzyl)-6, 7-dihydroxy-1, 2, 3, 4-tetrahydroisoquinoline containing catechol ring and tetrahydroisoquinoline nucleus in its own structure, both of which are well known to have agonistic effects on adrenergic receptors. Using guinea-pig atria(rich in ${\beta}_1$-receptor) and treachea(rich in ${\beta}_2$-receptor), we studied pharmacological actions of higenamine on these organs with special interest of its relevancy of ${\beta}$-receptor selectivity. In order to further clarify its pharmacological characteristics, the influncences of pretreatment of reserpine or cocaine were also investigated. The results were summarized as follows : 1. Higenamine had remarkable chronotropic, inotropic and bronchodilator effects in guinea-pig spontaneously beating right atria, left atria and trachea, in dose-dependent manners. 2. All of above actions were blocked competitively by propranolol, which shows nonselectivity of higenamine on ${\beta}$-receptor. $pA_2$ values of propranolol against higenamine were 7.93, 7.76 and 8.46 in guinea-pig right atria, left atria and treachea, respectively. 3. Reserpine pretreatment(5mg/kg, ip, 24h) did not show my decrease in pharmacological actions of higenamine, which suggests higenamine has direct action on ${\beta}$-receptor not via catecholamine release. 4. Cocaine pretreatment$(1{\mu}M)$ had no influence on pharmacological actions of higenamine in contrast with nor epinephrine, which suggests there is no neuronal uptake mechanism of higenamine in the studied organ preparations.

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A network pharmacology approach to explore the potential role of Panax ginseng on exercise performance

  • Kim, Jisu;Lee, Kang Pa;Kim, Myoung-Ryu;Kim, Bom Sahn;Moon, Byung Seok;Shin, Chul Ho;Baek, Suji;Hong, Bok Sil
    • Korean Journal of Exercise Nutrition
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    • v.25 no.3
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    • pp.28-35
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    • 2021
  • [Purpose] As Panax ginseng C. A. Meyer (ginseng) exhibits various physiological activities and is associated with exercise, we investigated the potential active components of ginseng and related target genes through network pharmacological analysis. Additionally, we analyzed the association between ginseng-related genes, such as the G-protein-coupled receptors (GPCRs), and improved exercise capacity. [Methods] Active compounds in ginseng and the related target genes were searched in the Traditional Chinese Medicine Database and Analysis Platform (TCMSP). Gene ontology functional analysis was performed to identify biological processes related to the collected genes, and a compound-target network was visualized using Cytoscape 3.7.2. [Results] A total of 21 ginseng active compounds were detected, and 110 targets regulated by 17 active substances were identified. We found that the active compound protein was involved in the biological process of adrenergic receptor activity in 80%, G-protein-coupled neurotransmitter in 10%, and leucocyte adhesion to arteries in 10%. Additionally, the biological response centered on adrenergic receptor activity showed a close relationship with G protein through the beta-1 adrenergic receptor gene reactivity. [Conclusion] According to bioavailability analysis, ginseng comprises 21 active compounds. Furthermore, we investigated the ginseng-stimulated gene activation using ontology analysis. GPCR, a gene upregulated by ginseng, is positively correlated to exercise. Therefore, if a study on this factor is conducted, it will provide useful basic data for improving exercise performance and health.

Control of parturition time on Pig 4. Effect of prostaglandin $F_2{\alpha}$ on uterine smooth muscle motility (돼지 분만시기의 조절에 관하여 4. 자궁평활근의 운동성에 대한 Prostaglandin $F_2{\alpha}$의 영향)

  • 심철수;정성진;이양성;임종옥
    • Korean Journal of Veterinary Service
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    • v.18 no.3
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    • pp.29-35
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    • 1995
  • The effects of prostaglandin $F_2{\alpha}$ were investigated on the uterine smooth muscle motility in the pig. The results were summarized as follows : 1. Prostaglandin $F_2{\alpha}$ caused the contraction of the porcine uterine smooth muscle and the contractile responses increased between the concentration of prostaglandine $F_2{\alpha}$ $10^{-9}$ M and $5{\times}10^{-8}$ M with a dose-dependent manner. 2. The contractile response induced by prostaglandine $F_2{\alpha}$($10^{-8}$ M) was not blocked by pre-treatment with cholinergic receptor blocker, atropine ($10^{-6}$ M). 3. The contractile response induced by prostaglandine $F_2{\alpha}$(10$^{-8}$ M) was not blocked by pretreament with ${\alpha}$-adrenergic receptor blocker, phentolamine($10^{-6}$ M) and ${\beta}$-adrenergic receptor blocker, propranolol($10^{-6}$ M). From these results, it was concluded that the effects of uterine smooth muscle by prostaglandine $F_2{\alpha}$ were only the contraction mediated by prostaglandine TEX>$F_2{\alpha}$ receptor in pig, and that it may not be related to the cholinergic and adrenergic receptor.

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Melanin-dispersing Effect of Vasopressin on Frog Skin Melanocyte (Vasopressin의 멜라닌 확산작용에 대하여)

  • Hong, Seung-Kil
    • The Korean Journal of Physiology
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    • v.7 no.2
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    • pp.59-66
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    • 1973
  • It has been reported that vasopressin disperse the melanophore granule of frog skin. The author used hypophysectomized and adrenergic receptor blockaded animals in order to define the mechanism of vasopressin on the melanopore pigment of frog skin. The Rana niglomaculata which could be found in the Seoul area were used on this experiment. The amount of the following drugs were injected into the lymphatic sac of the frog; vaospressin $(0.05\;{\mu}g/g\;B.W.)$, dibenzylin $(0.05\;{\mu}g/g\;B.W.)$, and propranolol $(0.01\;{\mu}g/g\;B.W.)$. The following results were observed; 1. Vasopressin dispersed the melanin granules of melanocyte of frog skin. 2. The melanin granule dispersion activity of vasopressin was observed on the hypophysectomized frog. 3. The melanin granule dispersion was observed on the adrenergic receptor blockaded frog with dibenzylin or propranolol respectively, especially the later one was found to be more obvious. 4. The melanin granule dispersion was observed on the frog which was injected with vasopressin after alpha-receptor or beta-receptor blockade and the later one was found to be more obvious. 5. The melanin granule dispersion was more effective with the blockade of beta-receptor after the treatment with vasopressin on hypophysectomized frog.

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