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�й�ҩѧ��־ 2008, Vol. 43 Issue (15) :1149-1152    DOI:
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1.����������ҽԺҩѧ�� ���� 100730;2.�й�ҽѧ��ѧԺ����Э��ҽѧԺҩ���о��� ���� 100050
LIU Zhi-jun1��ZHAO Ming2��CHEN Nai-hong2��ZHANG Jian-jun2
1.Department of Pharmacy��Beijing Hospital of Ministry of Health��Beijing 100730��China��2.Institute of Material Medica��Chinese Academy of Medical Sciences & Peking Union Medical College��Beijing 100050��China

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ժҪ Ŀ��ѡ����5-��ɫ��(5-HT)����ȡ���Ƽ�(selective serotonin reuptake inhibitors,SSRIs)��Ŀǰ�ٴ�Ӧ����㷺�����Ϳ�����ҩ�ͨ���������͡��������͡����̪�����������ֶ�5-HTת����(serotonin transporter,SERT)���������õ�ǿ��,Ϊ�ٴ�ѡ��ҩ���ṩʵ�����ݡ��������ô�����ͻ����ʹ���ѪС��SERT,ͨ���������ʵ��,�۲���SSRIs������SERT��[3H]5-HT����ȡ�仯,���IC50ֵ,�ȽϷ���͡��������͡����̪�����������ֶ�SERT�������õ�ǿ���������������֯ͻ�����ѪС��SERT�������������ʵ����ʾ,������͡������͡����̪�����������ֶ�SERT�������õ�IC50(nmol��L-1)�ֱ�Ϊ(ѪС��vsͻ����):(1.26vs 1.39)��(44.7vs 35.5)��(10.5vs 16.2)��(6.64vs 7.09)������4��SSRIs��SERT���������ö���ǿ,IC50��nmol��L-1���������������õ�ǿ������Ϊ������͡>������>��̪����>����͡��
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Abstract�� OBJECTIVE To investigate the strength of SSRIs' inhibitory effects on serotonin transporter,SERT and to offerprescription information for clinical therapy.METHODS The activity of SERT in rat synaptosomes and platelets was measured by determining the rate of [3H]5-HT accumulation under different concentration of paroxetine,fluoxetine,citalopram and sertraline.The IC50s of these SSRIs were calculated by linear regression.RESULTS The IC50s(platelet vs synaptosome)of paroxetine,fluoxetine,citalopram and sertraline were 1.26 vs 1.39,44.7 vs 35.5,10.5 vs 16.2 and 6.64 vs 7.09,respectively.CONCLUSION These widely used SSRIs have strong inhibitory effect on rat platelet and synaptosome SERT.Paroxetine has the most potent inhibitory effect and fluoxetine is the weakest one.
Keywords�� selective serotonin reuptake inhibitors,   serotonin transporter,   radioligand binding assay,   platelet,   synaptosome      
�ո�����: 2008-02-13;
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���ξ�, ����, ���˺�� .4���ٴ�����ѡ����5-��ɫ������ȡ���Ƽ���5-��ɫ��ת������������ñȽ�[J]  �й�ҩѧ��־, 2008,V43(15): 1149-1152
LIU Zhi-jun, ZHAO Ming, CHEN Nai-hong etc .In Vitro Comparison of Four SSRIs' Inhibitory Effect on Serotonin Transport [J]  Chinese Pharmaceutical Journal, 2008,V43(15): 1149-1152
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