• Title/Summary/Keyword: dopamine receptor

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A Bal I RFLP of Dopamine D3 Receptor Gene in Korean Hypertensives

  • Jang, Dai-Ho;Kim, Seoun-Jeong;Kang, Byung-Yong;Kim, Hyun-Hee;Lee, Kong-Oh
    • Environmental Mutagens and Carcinogens
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    • v.23 no.1
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    • pp.7-10
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    • 2003
  • Hypertension is characterized by multiple genetic and environmental factors. To establish the genetic basis of hypertension in Koreans, we investigated the genetic variations of dopamine D3 receptor (DRD3) gene in the Korean patients with hypertension and normotensive controls. There were no significant differences in the genotype and allele frequencies of Bal I RFLP in the DRD3 gene between two groups, respectively (P > 0.05). Our finding shows lack of association between a genetic marker of DRD3 gene and hypertension, suggesting that the genetic variation of DRD3 gene does not playa major role in the determination of hypertension in Korean population. Further studies in other ethnic groups will be required.

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Evaluation on the Abuse Liability of Ephedrine Using Rats (흰쥐를 이용한 에페드린의 약물남용가능성 평가)

  • 류승렬;김혜진;홍진태;이종권;이선희;이병무;김부영
    • YAKHAK HOEJI
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    • v.43 no.5
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    • pp.682-688
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    • 1999
  • Abuse liability of ephedrine was investigated by measurement of locomotor activity and self-administration in Sprague-Dawley rats. Locomotor activity was determined in rats treated with 3, 10 and 30 mg/kg ephedrine for 14 days. Self-administration by ephedrine (0.23, 1 and 2.3 mg/kg) was examined in food-trained rats. We also examined effect of dopamine receptor antagonist (spiperone, $30{\;}\mu\textrm{g}/kg$) on the ephedrine-induced response of self-administration. Body weight was not statistically difference between control and ephedrine treatment group, but locomotor activity was dose-dependently increased. Self-administration for ephedrine was decreased in the early response (day 1 and 2) but the response was increased by higher dose of ephedrine. Self-administration was decreased by dopamine receptor antagonist (spiperone). These data showed that ephedrine increased locomotor activity and induced response of self-administration, and the effects of ephedrine were partially related to the dopaminergic system, which suggest the ephedrine may have abuse liability.

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Effects of the dopaminergic system on release of TSH and thyroid hormone in rats (랫드에서 TSH와 갑상선 호르몬에 미치는 dopamine계의 영향)

  • Lee, Sang-woo;Kim, Jin-sang;Han, Jeong-hee
    • Korean Journal of Veterinary Research
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    • v.32 no.2
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    • pp.165-173
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    • 1992
  • The present study was carried out to investigate the effects of dopaminergic drugs and the role of specific dopamine(DA) receptors on the release of TSH, $T_4$ and $T_3$. Serum TSH levels (cold-induced, $4{^{\circ}C}$) were determined using RIA(radioimmunoassay) at 30 min after administration of dopamine agonists and antagonists. Serum $T_4$ and $T_3$ levels were detected after these dopaminergic drugs were administered subcutaneously twice a day for a week. The results of the study are summarized as follows : Apomorphine, a nonspecific DA receptor agonist, produced a dose-depedent decrease in serum TSH, $T_4$ and $T_3$ levels. However, only low doses (0.3, 1.0mg/kg) of SKF38393, a specific $D_1$-receptor agonist, produced a decrease in serum lelvels of TSH. I,Y171555, a specific $D_2$-receptor agonist, produced a dose dependent decrease in serum TSH, $T_4$ and $T_3$ levels. However, SCH23390, a specific $D_1$-receptor antagonist, produced a decrease except in serum T levels which were increased dose dependently. High doses (1.0, 3.0mg/kg) of sulpiride, a specific $D_2$-receptor antagonist, made a increase in the serum levels of TSH and $T_3$. The effects of dopaminergic drugs in serum TSH and $T_4$ levels was potentiated by the pretreatment of apomorphine. The overall results of this study suggest that the regulation of TSH, $T_4$ and $T_3$ secretion were mediated via specific $D_1$ and $D_2$ receptor.

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Dopaminergic Inhibition of Dorsal Horn Cell Activity in the Cat

  • Kim, Kyung-Chul;Shin, Hong-Kee;Kim, Kee-Soon
    • The Korean Journal of Physiology and Pharmacology
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    • v.2 no.6
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    • pp.661-670
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    • 1998
  • Dopamine has been generally known to exert antinociceptive action in behavioral pain test, such as tail flick and hot plate test, but there appears to be a great variance in the reports on the antinociceptive effect of dopamine depending on the dosage and route of drug administration and type of animal preparation. In the present study, the effects of dopamine on the responses of wide dynamic range (WDR) cells to mechanical, thermal and graded electrical stimuli were investigated, and the dopamine-induced changes in WDR cell responses were compared between animals with an intact spinal cord and the spinal animals. Spinal application of dopamine (1.3 & 2.6 mM) produced a dose-dependent inhibiton of WDR cell responses to afferent inputs, the pinch-induced or the C-fiber evoked responses being more strongly depressed than the brush-induced or the A-fiber evoked responses. The dopamine-induced inhibition was more pronounced in the spinal cat than in the cat with intact spinal cord. The responses of WDR cell to thermal stimulation were also strongly inhibited. Dopamine $D_2$ receptor antagonist, sulpiride, but not $D_1$ receptor antagonist, significantly blocked the inhibitory action of dopamine on the C-fiber and thermal responses of dorsal horn cells. These findings suggest that dopamine strongly suppresses the responses of WDR cells to afferent signals mainly through spinal dopamine $D_2$ receptors and that spinal dopaminergic processes are under the tonic inhibitory action of the descending supraspinal pathways.

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Radioligands for Imaging Dopamine and Serotonin Receptors and Transporters (도파민과 세로토닌 운반체 및 수용체 영상을 위한 방사성리간드)

  • Chi, Dae-Yoon
    • The Korean Journal of Nuclear Medicine
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    • v.34 no.3
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    • pp.159-168
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    • 2000
  • In the 1980s, techniques to image the human subjects in a three-dimensional direction were developed. Two major techniques are SPECT (Single Photon Emission Computed Tomography) and PET (Positron Emission Tomography) which allow the detector to detect a single photon or annihilation photons emitted from the subjects injected with radiopharmaceuticals. Since the latter two techniques can measure the density of receptors, enzymes and transporters in living human, it may be very important project to develop selective methods of labeling with radionuclides and to develop new radiopharmaceuticals. There has been a considerable interest in developing new compounds which specifically bind to dopamine and serotonin receptor and transporters, and it will be thus very useful to label those compounds with radionuclides in order to gain a better understanding in biochemical and pharmacological interactions in living human. This review mentions the characteristics of radioligands for the imaging of dopamine and serotonin receptors and transporters. Although significant progress has been achieved in the development of new PET and SPECT ligands for in vivo imaging of those receptors and transporters, there are continuous needs of new diagnostic radioligands.

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Dopamine Transporter Gene and Dopamine D2, D3, D4 Receptor Gene Polymorphisms in Attention Deficit Hyperactivity Disorder (주의력결핍 과잉행동장애에서 도파민 전달체 및 도파민 D2, D3, D4 수용체 유전자 다형성)

  • Park, Pil-Sang;Kim, Dae-Kwang;Jung, Chul-Ho
    • Journal of the Korean Academy of Child and Adolescent Psychiatry
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    • v.19 no.1
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    • pp.19-27
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    • 2008
  • Objectives : The aim of this study was to examine the association of attention-deficit hyperactivity disorder (ADHD) in Korean populations with functional polymorphisms of six genes dopamine receptors (Ser311/Cys311 polymorphism, Taq1 A polymorphism, and Taq1 B polymorphism in DRD2, BalI polymorphism in DRD3, and promoter -521 C/T polymorphism and exon III 48 bp repeat polymorphism in DRD4) and one gene in dopamine transporter (DAT1). Methods : Participants were 58 children with ADHD and 110 control children. The genotypes were determined by PCR. Results : There was a statistically significant difference in genotype frequency of -521 C/T polymorphism within the promoter region of the DRD4 between two groups. Furthermore, in the male group, both genotype and allele frequencies showed statistically significant differences. Conclusion : Findings of the study indicate that -521 C/T polymorphism in promoter region of DRD4 appears to be a possible candidate gene for ADHD in Korean population.

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An in Vivo Study of Dopamine Metabolism in Hyperglycemic Rat Striatum

  • Lim, Dong-Koo;Lee, Kyung-Min
    • Archives of Pharmacal Research
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    • v.18 no.4
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    • pp.249-255
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    • 1995
  • The changes in the levels of the extracellular dopamine metabolites and the responses to various dopamine agents were studied by using microdialysis inhyperglycemic rat striatum. The hyperglycemia were induced by the administriation of streptozotocin (40 mg/kg, i.p. for 3 days.). The basal levels of striatal dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) were significantly decreased in hyperglycemic rat striatum. After the administration ofl D-1 and D-2 receptor antagonists, SCH-23390 and (-)sulpiride, to rats 14 days after the last administration of STZ, the increased rates in DOPAC levels were higher in hyper- than in normoglycemic rats. However, after the administration of dopamine autoeceptor agonist, 3(-)PPP, the levels of the extracellular HVA were increased in normoglycemic rats, but those were not altered in hyperglycemic rats. The results indicate that the striatal dopamine activities were decreased in the hyperglycemic rats and suggest that release of dopamine may be decreased in hyperglycemic rats. Furthermore it suggest that the increase in the levels of the extracellular dopamine metabolites by dopamine antagonists might be dur to the incrrased sensitivities of the dopamine receptors in hyperglycemic state.

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Lack of Association Between the Dopamine $D_3$ Receptor Gene and Korean Schizophrenic Patients (한국인 정신분열증 환자와 도파민 $D_3$ 수용체 유전자의 연합)

  • Han, Moon-Cyun;Lee, Min-Soo;Lee, Dae-Hie
    • Korean Journal of Biological Psychiatry
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    • v.2 no.2
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    • pp.237-247
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    • 1995
  • The finding of contrasting results regarding an association between schizophrenia and the Mlul polymorphism site in the dopamine $D_3$ receptor gene prompted us to study the distribution of this palymorphism in Korean schizophrenic patients and controls. The author's approach was case-control study. Schizophrenic patients (n=66) and controls (n=76) were examined by case-control study for distribution of the Mlul polymorphism of the dopamine $D_3$ receptor gene in Korean population to minimize the effect of racial differencies in gene frequencies. The frequency of the allele 1 in schizophrenic patients and controls was 0.66 and 0.76, respectively. There was no significant differencies in the frequency of the allele 1 between schizophrenic patients and controls ($x^2$=3.07, p>.05), and between positive and negative schizophrenic patients ($x^2$=1.02, p>.05). We present here the evidence of a lack of alleic association between the Mlul polymorphism of the dopamine $D_3$ receptor gene and Korean schizophrenic patients and also report no increased homozygosity for the Mlul polymorphism. The assumption that the dopamine $D_3$ receptor gene has a predisposing role in schizophrenia was not supported by this case-control study. Although, the possibility that this gene has a minor gene effects in the etiology of schizophrenia cannot be excluded because of the intrinsic limitations of the methods of analysis and number of subjects in our study.

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Studies on the Adrenergic Alpha-Receptor in the Guinea Pig Ileum (해명 회장 운동에 대한 아드레나린성 ${\alpha}$-수용체에 관한 연구)

  • Ko, Chang-Mann
    • The Korean Journal of Pharmacology
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    • v.19 no.1
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    • pp.85-92
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    • 1983
  • Intestine is innervated by an interconnected plexus of both sympathetic and parasympathetic nerve fibers. Sympathetic influence causes inhibition of intestinal motility mediated by both ${\alpha}-\;and\;{\beta}-adrenergic$ receptors. The mechanism of intestinal relaxation by ${\beta}-receptors$ has been extensively studied, but the function of ${\alpha}-receptors$ in intestinal motility is still unclear. Although it is suggested that catecholamine reduces acetylcholine release and this may play an important role in ${\alpha}-receptor$ mediated intestinal relaxation, there is no definite evidences about the mechanism and site of action of ${\alpha}-receptor$ mediated relaxation. In this experiment, therefore, the effect and site of action of ${\alpha}-receptor$ agonists were investigated in the guinea pig ileum using electrical field stimulation. The results are summarized as follows : 1) Electrical field stimulation elicited tonic contraction in isolated guinea pig ileum ana this contraction was completely inhibited by the pretreatment of tetrodotoxin or atropine. 2) Norepinephrine, epinephrine and dopamine inhibited the contraction induced by electrical field stimulation but methoxamine and phenylephrine had little effects. 3) Inhibitory effects of norepinephrine and dopamine was partially blocked by yohimbine and phentolamine pretreatment. But haloperidol and propranolol pretreatment cause no effects on the electrical field stimulation induced contraction. Inhibitory effect of dopamine was completely blocked by both haloperidol and yohimbine pretreatment. 4) Inhibitory effects of norepinephrine and dopamine were little affected by the pretreatment with hexamethonium. It is suggested that electrical field stimulation causes tonic contraction of guinea pig ileum by releasing acetylcholine from postganglionic fiber, and this release is blocked by presynaptic ${\alpha}-receptor$ activation.

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Three-dimensional Pharmacophore Mapping of a Series of Isoxazolylpiperazine Inhibitors Selectively acting on the Dopamine D4 Receptor

  • Pae, Ae-Nim;Lee, In-Young;Koh, Hun-Yeong
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.183-185
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    • 2002
  • The discovery of new ligands with affinity and selectivity for the dopamine $D_2$ receptor subtypes is an important area in medicinal chemistry. The distribution of the $D_2$ receptors in the limbic areas of brain suggests that these receptors may be particularly an attractive target for the design of potential selective antipsychotic drugs without causing extrapyramidal side effects. (omitted)

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