• Title/Summary/Keyword: Dopamine receptor D2

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Interrelationship between Dopaminergic Receptors and Catecholamine Secretion from the Rat Adrenal Gland (흰쥐 부신에서 카테콜아민 분비작용과 도파민 수용체간의 상관성)

  • Lim, Dong-Yoon;Yoon, Joong-Keun;Moon, Baek
    • The Korean Journal of Pharmacology
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    • v.30 no.1
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    • pp.87-100
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    • 1994
  • It has been known for some time that dopamine-containing cells are existed in sympathetic ganglia, i.e., small, intensely fluorescent cells. However, its role and mechanism of action as a peripheral neurotransmitter are poorly understood so far. In the present study, an attempt was made to examine the effect of apomorphine, which is known to be a selective agonist of dopaminergic $D_2$. receptor on secretion of catecholamines (CA) from the isolated perfused rat adrenal gland. The perfusion of a low concentration of 10uM apomorphine into an adrenal vein for 20 min produced significant reduction in CA secretion induced by 5.32 mM ACh, 56 mM KCl, 100 uM DMPP and 100 uM McN-A-343. Increasing apomorphine concentration to 30 uM led to more markedly decreased CA secretion as compared to the case of 10 uM apomorphine and also did inhibit clearly CA release by $10^{-5}M$ Bay-K-8644. Furthermore, in adrenal glands preloaded with a higher dose of 100 uM apomorphine, CA releases evoked by ACh, excess $K^+$, DMPP and McN-A-343 were almost abolished by the drug. The perfusion of $3.3{\pm}10^{-5}M$ metoclopramide, which is well-known as a selective dopaminergic $D_2$ antagonist, produced significantly inhibitory effect of CA release by ACh, DMPP and McN-A-343 but did not affect that by excess $K^+$. However, preloading of 30uM apomorphine in the presence of metoclopramide did not modify the CA secretory effect of excess $K+$ and DMPP. These experimental results demonstrate that apomorphine causes dose-dependent inhibition of CA secretion by cholinergic receptor stimulation and also by membrane depolarization from the isolated perfused rat adrenal gland, suggesting that these effects appear to be exerted by inhibiting influx of extracellular calcium into the rat adrenal medullary chromaffin cells through activation of inhibitory dopaminergic receptors.

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A study of Brain Micro-PET Imaging and Bindingpotential with a Different Specific Activity of 18F-Fallypride in the Small Animal (소동물에서 18F-Fallypride의 비방사능에 따른 뇌의 PET이미지와 Binding Potential 차이에 대한 연구)

  • Cho, Kyu-Sang;Ahn, Sung-Min
    • The Journal of the Korea Contents Association
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    • v.15 no.9
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    • pp.418-424
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    • 2015
  • In this study, we proceed if there are any changes in binding ability of receptor-ligand in some degree of SA and in radioactive uptake from the corpus striatum based on small animal experiment in vivo based on the S.A values. By dividing 18F-Fallypride into 3 S.A values(high S.A : 43.29~74 GBq/umol, ordinary S.A : 20.72~29.23 GBq/umol, low S.A : 6.29~8.51 GBq/umol), we injected directly into the veins and performed 90 minutes of dynamic scan using Micro PET. After scanning, we compared and analyzed with Binding Potential (Binding Potential) from the bilateral striatum. high SA and low SA, ordinary SA and low SA showed significant differences. Also, in the image comparison using 18F-Fallypride show high radioactive uptake in the striatum at high SA and ordinary SA, but the radioactive uptake at low SA is lower than other two SA. Since 18F-Fallypride has affinity to dopamine D2/3 pharmacokinetic, the difference of Binding Potentials at decreased level of SA values was not that significant. However, further PET research of the corpus striatum using 18F-Fallypride is necessary because the differences in images and Binding Potentials at 6.5 times smaller SA values compared to high SA value showed were significant.

Association Study between Treatment Response of Amisulpride and Dopamine D3 Receptor Gene Polymorphisms (조현병 환자에서 아미설프라이드의 치료반응과 도파민 D3 수용체 유전자다형성의 연관성)

  • Kang, Seung-Gul;Lee, Heon-Jeong;Lee, Seung Jae;Choi, Tae Young;Woo, Jungmin;Kim, Jihyun;Jung, Sung-Won;Koo, Bon Hoon;Lee, Kwanghun;Kim, Jeong-Lan;Chee, Ik-Seung;Lee, Jonghun
    • Korean Journal of Biological Psychiatry
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    • v.20 no.3
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    • pp.91-96
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    • 2013
  • Objectives The aim of this study is to evaluate the association between rs6280 and rs905568 genetic polymorphism of DRD3 gene and the treatment response of amisulpride. Methods After six weeks treatment of amisulpride, 125 schizophrenia patients were interviewed based on the Positive and Negative Syndrome Scale (PANSS) and the Clinical Global Impression-Severity (CGI-S). The genotyping for rs6280 and rs905568 was performed using TaqMan single nucleotide polymorphism (SNP) genotyping assay. Results There was no significant difference in the frequency of genotype and allele of rs6280 between the responders and non-responders based on the total, positive, and general score of PANSS and CGI-S score. However, there was a significant association between this SNP and treatment response in the negative score of PANSS (${\chi}^2=5.23$, p = 0.022). There was no significant association between rs905568 and the response in positive, negative, general, and total PANSS score and CGI-S score. Conclusions This is the first positive association study between DRD3 gene and the treatment response of negative symptoms to amisulpride in Korean schizophrenia patients. A larger scale research on more SNP of the DRD3 gene will make a progress in the study of pharmacogenetics on the treatment response of the amisulpride.