Antidepresan trisiklik
Farmakologi > Profil pengikatan

Profil pengikatan berbagai TCA dan beberapa metabolit dalam hal afinitasnya (Ki, nM) untuk berbagai reseptor dan transporter adalah sebagai berikut:
| Senyawa | SERT | NET | DAT | 5-HT1A | 5-HT2A | 5-HT2C | 5-HT6 | 5-HT7 | α1 | α2 | D2 | H1 | H2 | mACh | σ1 | σ2 |
| --- | --- | --- | --- | --- | --- | --- | --- | --- | --- | --- | --- | --- | --- | --- | --- | --- |
| Amineptin | >100.000 | 10.000 | 1.000–1.400 | >100.000 | 74.000 | ND | ND | ND | >100.000 | >100.000 | >100.000 | ≥13.000 | ND | >100.000 | ND | ND |
| Amitriptilin | 2,8–4,3 | 19–35 | 3.250 | ≥450 | 18–23 | 4,0 | 65–141 | 93–123 | 4.4–24 | 114–690 | 196–1.460 | 0,5–1,1 | 66 | 9,6 | 300 | ND |
| Amoksapin | 58 | 16 | 4.310 | ND | 0,5 | 2,0 | 6,0–50 | 41 | 50 | 2.600 | 3,6–160 | 7,9–25 | ND | 1.000 | ND | ND |
| Butriptilin | ≥1.360 | 5.100 | 3.940 | 7.000 | 380 | ND | ND | ND | 570 | 4.800 | ND | 1,1 | ND | 35 | ND | ND |
| Klomipramin | 0,14–0,28 | 38–54 | ≥2.190 | ≥7.000 | 27–36 | 65 | 54 | 127 | 3,2–38 | ≥535 | 78–190 | 13–31 | 209 | 37 | 546 | ND |
| Desipramin | 18–163 | 0,63–3,5 | 3.190 | ≥6.400 | 115–350 | 244–748 | ND | >1.000 | 23–130 | ≥1.379 | 3.400 | 60–110 | 1.550 | 66–198 | ≥1.990 | ≥1.610 |
| Dibenzepin | ND | ND | >10.000 | >10.000 | ≥1.500 | ND | ND | ND | >10.000 | >10.000 | >10.000 | 23 | 1.950 | 1.750 | ND | ND |
| Dosulepin | 8,6–78 | 46–70 | 5.310 | 4.000 | 152 | ND | ND | ND | 419 | 2.400 | ND | 3,6–4,0 | ND | 25–26 | ND | ND |
| Doksepin | 68–210 | 13–58 | ≥4.600 | 276 | 11–27 | 8,8–200 | 136 | ND | 24 | 28–1.270 | 360 | 0,09–1,23 | 174 | 23–80 | ND | ND |
| Imipramin | 1,3–1,4 | 20–37 | 8.500 | ≥5.800 | 80–150 | 120 | 190–209 | >1.000 | 32 | 3.100 | 620–726 | 7,6–37 | 550 | 46 | 332–520 | 327–2.100 |
| Iprindola | ≥1.620 | 1.260 | 6.530 | 2.800 | 217–280 | 206 | ND | ND | 2.300 | 8.600 | 6.300 | 100–130 | 200–8.300 | 2.100 | >10,000 | ND |
| Lofepramin | 70 | 5,4 | >10.000 | 4.600 | 200 | ND | ND | ND | 100 | 2.700 | 2.000 | 245–360 | 4.270 | 67 | 2.520 | ND |
| Maprotilin | 5.800 | 11–12 | 1.000 | ND | 51 | 122 | ND | 50 | 90 | 9.400 | 350–665 | 0,79–2,0 | 776 | 570 | ND | ND |
| Norklomipramin | 40 | 0,45 | 2.100 | 19.000 | 130 | ND | ND | ND | 190 | 1.800 | 1.200 | 450 | ND | 92 | ND | ND |
| Nortiaden | 192 | 25 | 2.539 | 2.623 | 141 | ND | ND | ND | 950 | ND | ND | 25 | ND | 110 | ND | ND |
| Nortriptilin | 15–18 | 1,8–4,4 | 1.140 | 294 | 5,0–41 | 8,5 | 148 | ND | 55 | 2.030 | 2.570 | 3,0–15 | 646 | 37 | 2.000 | ND |
| Opipramol | ≥2.200 | ≥700 | ≥3.000 | >10.000 | 120 | ND | ND | ND | 200 | 6.100 | 120–300 | 6,0 | 4.470 | 3.300 | 0,2–50 | 110 |
| Protriptilin | 19,6 | 1,41 | 2.100 | 3.800 | 70 | ND | ND | ND | 130 | 6.600 | 2.300 | 7,2–25 | 398 | 25 | ND | ND |
Tianeptin: >10.000
| Trimipramin | 149–2.110 | ≥2.450 | ≥3.780 | 8.000 | 32 | 537 | ND | ND | 24 | 680 | 143–210 | 0,27–1,5 | 41 | 58 | ND | ND |
Nilainya adalah Ki (nM). Semakin kecil nilainya, semakin kuat obat tersebut terikat pada lokasi tersebut. Untuk spesies dan referensi pengujian, lihat artikel obat masing-masing. Sebagian besar, tetapi tidak semua nilai, adalah untuk protein manusia.
Kecuali reseptor sigma, TCA bertindak sebagai antagonis reseptor atau agonis terbalik reseptor dan sebagai penghambat transporter. Tianeptin termasuk dalam daftar ini karena secara teknis merupakan TCA, tetapi dengan farmakologi yang sangat berbeda.
Kadar terapeutik TCA umumnya berada dalam kisaran sekitar 100 hingga 300 ng/mL, atau 350 hingga 1.100 nM. Pengikatan protein plasma umumnya 90% atau lebih.