• Title/Summary/Keyword: [$^3H$]Imipramine 결합

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REPEATED AGGRESSIVE BEHAVIOR AND PLATELET $^3H$ IMIPRAMINE BINDING (반복적인 공격적 행동과 혈소판 $^3H$ Imipramine 결합의 상관관계 연구)

  • Choi, Jin-Sook;Woo, Jong-In;Hong, Kang-E
    • Journal of the Korean Academy of Child and Adolescent Psychiatry
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    • v.5 no.1
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    • pp.93-101
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    • 1994
  • This study was performed to assess the amount of altered serotonergic responsivity in individuals with repeated aggressive behaviors compared with normal controls. Sixteen aggressive(delinquent criminals with repeated aggressive behaviors) and seventeen controls(medical college students) were selected and assessed their severity of aggression by several psychological instruments. The platelet $^3H$-imipramine binding sites which is known to correlate the serotonergic function of the central nervous system were measured. The results are as follows. 1) Mean scores of physical aggression in the aggressive subjects were found to be significantly higher than normal controls(p<.01). And impulsivity, hostility, psychoticism in the aggressives were found higher than controls, also. 2) In the paltelet $^3H$-imipramine binding, the aggressives had a tendency of reduced maximal binding sites(Bmax) comparing with controls(p=.0841). 3) There was no statistically significant differences between two groups in the binding coefficients(Kd) of platelet $^3H$ Imipramine binding. 4) The value of maximal binding sites(Bmax) showed significant inverse correlations with aggressive scale scores of PFAV(r=-.6311), and physical aggression scale scores of CTS(r=-.5377).

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Effects of Chronic Treatments with 5-HT Uptake Inhibitors on the [$^3H$]Imipraine and [$^3H$]Paroxetine Binding, [$^3H$]5-HT Uptake, and 5-HT Content of the Rabbit Platelet (5-HT 흡수억제성 항우울제들이 가토혈소판의 [$^3H$]Imipramine과 [$^3H$]Paroxetine Binding, [$^3H$]5-HT 흡수, 및 5-HT함량에 미치는 영향)

  • Won, Kyong-Sik;Lee, Min-Soo;Shin, Kyung-Ho;Chun, Boe-Gwun;Kwak, Dong-Il
    • Korean Journal of Biological Psychiatry
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    • v.1 no.1
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    • pp.88-97
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    • 1994
  • Many evidences are compatible with the correlation between the inhibition of [$^3H$] imipramine([$^3H$]IMI) and [$^3H$]paroxetine([$^3H$]PAT) binding to the 5-hydroxytryptamine(5-HT) transporter complex and the 5-HT uptake of 5-HT neurons and platelets, and most antidepressants have been shown to inhibit the [$^3H$]IMI and [$^3H$]PAT binding and the neuronal 5-HT uptake. However, several paradoxical research findings led to doubt about the pharmacological significance of the [$^3H$]IMI and [$^3H$]PAT binding sites. This study was carried to clarify the correlation between the [$^3H$]IMI and [$^3H$]PAT binding parameters and the tissue 5-HT content or/and [$^3H$]5-HT uptake in the rabbit platelet, which contains 40 times ad much 5-HT as that of human platelet and shows the 10 fold higher $B_{max}$ of the 5-HT transporter binding to a 5-HT uptake inhibitor. The rabbits were treated for 28 days with amitriptyline(4mg/kg/day : AP), fluoxetine(0.5mg/kg/day : FO), and sertraline(0.5mg/kg/day : SA) via an Alzet osmotic pump implanted for constant infusion. The [$^3H$]IMI binding $B_{max}$ and $K_d$ of the rabbit platelets were $6.4{\pm}1.2$pmol/mg protein and $10.9{\pm}2.1$nM and those in the [$^3H$]PAT binding were $8.6{\pm}1.1$pmol/mg protein and $1.6{\pm}0.3$nM, respectively. AP slightly increased $B_{max}$ of [$^3H$]IMI binding and both [$^3H$]IMI binding and [$^3H$]PAT binding $K_d$, and i contrast, it slightly decreased $B_{max}$ of [$^3H$]PAT binding. FO Slightly increased $K_d$ of both and [$^3H$]IMI and [$^3H$]PAT binding and slightly decreased $B_{max}$ of [$^3H$]IMI and [$^3H$]PAT binding. SA produced the significant increase of [$^3H$]PAT binding $B_{max}$ and the slight increase of both [$^3H$]IMI and [$^3H$]PAT binding $K_d$ and in contrast, it slightly decreased $B_{max}$ and of [$^3H$]IMI binding. And, the $V_{max}$ and $K_m$ of platelet [$^3H$]5-HT uptake were $24.2{\pm}2.4$pmol/$10^8$ platelets/min and $3.3{\pm}0.3$nM, respectively. The $V_{max}$ was little affected by AP, FO, or SA, but the [$^3H$]5-HT uptake $K_m$ value was moderately increased by FO. However, the platelet 5-HT content was moderately decreased by all of the 5-HT uptake inhibitors used in this study. These results seem to be consistent with the allosterical and competitive interaction of 5-HT uptake inhibiting antidepressants with each other as well as 5-HT in the 5-HT transporter binding, and provide no support for the view that the potencies of 5-HT uptake inhibitors to inhibit the [$^3H$]IMI or [$^3H$]PAT binding with 5-HT transporter complex correlate with their antidepressant potencies.

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