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ويقومُ الأَميتريبتيلين على زيادة تَركيز السيروتونين والنورأدرينالين (من الموادِّ الكيميائيَّة التي تُحفِّز الخلايا العصبية)، وعرقلة عمل موادَّ كيميائيَّة أخرى في المخ إلى حدٍّ أقل، لاسيَّما الأسيتيل كولين؛ فعندما يجري إفرازُ السيروتونين والنُّورأدرينالين من الخلايا العصبيَّة في الدِّماغ تعمل على التخفيف من الحالة المزاجية.
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