Aripiprazole
Site |
Ki (nM) |
Action |
5-HT1A |
1.7–5.6 |
Partial agonist |
5-HT1B |
830 |
ND |
5-HT1D |
68 |
ND |
5-HT1E |
8,000 |
ND |
5-HT2A |
3.4–35 |
Antagonist |
5-HT2B |
0.36 |
Inverse agonist |
5-HT2C |
15–180 |
Partial agonist |
5-HT3 |
628 |
ND |
5-HT5A |
1,240 |
ND |
5-HT6 |
214–786 |
Antagonist |
5-HT7 |
9.6–39 |
Antagonist |
D1 |
265–1,170 |
ND |
D2 |
0.45–3.3 |
Partial agonist |
D2L |
0.34–0.74 |
Partial agonist |
D3 |
0.8–9.7 |
Partial agonist |
D4 |
44–514 |
Partial agonist |
D5 |
95–2,590 |
ND |
α1A |
25.9 |
ND |
α1B |
34.4 |
ND |
α2A |
74.3 |
ND |
α2B |
102 |
ND |
α2C |
37.9 |
ND |
β1 |
141 |
ND |
β2 |
163 |
ND |
H1 |
27.9–61 |
ND |
H2 |
>10,000 |
ND |
H3 |
224 |
ND |
H4 |
>10,000 |
ND |
M1 |
6,780 |
ND |
M2 |
3,510 |
ND |
M3 |
4,680 |
ND |
M4 |
1,520 |
ND |
M5 |
2,330 |
ND |
SERT |
98–1,080 |
Blocker |
NET |
2,090 |
Blocker |
DAT |
3,220 |
Blocker |
NMDA (PCP) |
4,001 |
Antagonist |
|
Zyprexa
Site |
Ki (nM) |
Action |
5-HT1A |
2,063–2,720 |
Antagonist |
5-HT1B |
509–660 |
ND |
5-HT1D |
540–1,582 |
ND |
5-HT1E |
2,010–2,408 |
ND |
5-HT1F |
310 |
ND |
5-HT2A |
1.32–24.2 |
Inverse agonist |
5-HT2B |
11.8–12.0 |
Inverse agonist |
5-HT2C |
6.4–29 |
Inverse agonist |
5-HT3 |
202 |
Antagonist |
5-HT5A |
1,212 |
Full Agonist |
5-HT6 |
6.0–42 |
Antagonist |
5-HT7 |
105–365 |
Antagonist |
α1A |
109–115 |
Antagonist |
α1B |
263 |
Antagonist |
α2A |
192–470 |
Antagonist |
α2B |
82–180 |
Antagonist |
α2C |
29–210 |
Antagonist |
β1 |
>10,000 |
ND |
β2 |
>10,000 |
ND |
D1 |
35–118 |
Antagonist |
D2 |
3.00–106 |
Antagonist |
D2L |
31–38 |
Antagonist |
D2S |
21–52 |
Antagonist |
D3 |
7.8–91 |
Antagonist |
D4 |
1.6–50 |
Antagonist |
D4.2 |
17–102 |
Antagonist |
D4.4 |
21–60 |
Antagonist |
D5 |
74–90 |
Antagonist |
H1 |
0.65–4.9 |
Inverse agonist |
H2 |
44 |
Antagonist |
H3 |
3,713 |
Antagonist |
H4 |
>10,000 |
Antagonist |
M1 |
2.5–73 |
Antagonist |
M2 |
48–622 |
Antagonist |
M3 |
13–126 |
Antagonist |
M4 |
10–350 |
Antagonist |
M5 |
6.0–82 |
Antagonist |
|
Vraylar/Cariprazine (squashed banana)
Site |
Ki (nM) |
Action
|
5-HT1A |
2.6 |
Partial agonist
|
5-HT2A |
18.8 |
Antagonist
|
5-HT2B |
0.58 |
Antagonist
|
5-HT2C |
134 |
Inverse agonist
|
5-HT7 |
111 |
Antagonist
|
α1A |
155 |
Antagonist
|
D2L |
0.49 |
Partial agonist
|
D2S |
0.69 |
Partial agonist
|
D3 |
0.085 |
Partial agonist
|
H1 |
23.2 |
Antagonist
|
mACh |
>1,000 |
Antagonist
|
|
Haldol
|
Cymbalta
|
Trazodone (and metabolite)[43]
Site |
Trazodone |
mCPP |
Species |
SERT |
160–>10,000[44] |
202–432 |
Human |
NET |
≥8,500 |
≥1,940 |
Human |
DAT |
≥7,400 |
ND |
Human |
5-HT1A |
96–118 |
44–400 |
Human |
5-HT1B |
>10,000 |
89–501 |
Human |
5-HT1D |
106 |
210–1,300 |
Human |
5-HT1E |
>10,000 |
ND |
Human |
5-HT1F |
ND |
ND |
ND |
5-HT2A |
20–45 |
32–398 |
Human |
5-HT2B |
74–189 |
3.2–63 |
Human |
5-HT2C |
224–402 |
3.4–251 |
Human |
5-HT3 |
>10,000 |
427 |
Human |
5-HT4 |
ND |
ND |
ND |
5-HT5A |
>10,000 |
1,354 |
Human |
5-HT6 |
>10,000 |
1,748 |
Human |
5-HT7 |
1,782 |
163 |
Human |
α1 |
12–42 |
97–2,900 |
Human |
α1A |
153 |
1,386 |
Human |
α1B |
ND |
915 |
Human |
α1D |
ND |
ND |
ND |
α2 |
106–490 |
112–570 |
Human |
α2A |
728 |
145 |
Human |
α2B |
ND |
106 |
Human |
α2C |
155 |
124 |
Human |
β |
>10,000 |
2,500 |
Human |
β1 |
>10,000 |
2,359 |
Human |
β2 |
>10,000 |
3,474 |
Human |
D1 |
3,730 |
7,000 |
Human |
D2 |
≥3,500 |
>10,000 |
Human |
D3 |
353 |
>10,000 |
Rat |
D4 |
703 |
ND |
Human |
D5 |
>10,000 |
>10,000 |
Human |
H1 |
220–1,100 |
326 |
Human |
H2 |
3,290 |
ND |
Human |
H3 |
>10,000 |
ND |
Guinea pig |
H4 |
>10,000 |
ND |
Human |
mAChRs |
>10,000 |
>10,000 |
Human |
nAChRs |
>10,000 |
>10,000 |
Human |
σ1 |
>10,000 |
ND |
Rat |
σ2 |
536 |
8,350 |
Rat |
I1 |
ND |
759 |
Rat |
NMDAR (MK-801) |
>10,000 |
ND |
Rat |
VDCCs |
>10,000 |
6,043 |
Rat |
|
Risperidone
Site |
Ki (nM) |
Action
|
5-HT1A |
423 |
Antagonist
|
5-HT1B |
14.9 |
Antagonist
|
5-HT1D |
84.6 |
Antagonist
|
5-HT2A |
0.17 |
Inverse agonist
|
5-HT2B |
61.9 |
Inverse agonist
|
5-HT2C |
12.0 |
Inverse agonist
|
5-HT5A |
206 |
Antagonist
|
5-HT6 |
2,060 |
Antagonist
|
5-HT7 |
6.60 |
Irreversible
antagonist |
α1A |
5.0 |
Antagonist
|
α1B |
9.0 |
Antagonist
|
α2A |
16.5 |
Antagonist
|
α2B |
108 |
Antagonist
|
α2C |
1.30 |
Antagonist
|
D1 |
244 |
Antagonist
|
D2 |
3.57 |
Antagonist
|
D2S |
4.73 |
Antagonist
|
D2L |
4.16 |
Antagonist
|
D3 |
3.6 |
Inverse agonist
|
D4 |
4.66 |
Antagonist
|
D5 |
290 |
Antagonist
|
H1 |
20.1 |
Inverse agonist
|
H2 |
120 |
Inverse agonist
|
mACh |
>10,000 |
Negligible
| |
benadryl/Diphenhydramine[44]
Site |
Ki (nM) |
Species |
Ref
|
SERT |
≥3,800 |
Human |
[45][46]
|
NET |
960–2,400 |
Human |
[45][46]
|
DAT |
1,100–2,200 |
Human |
[45][46]
|
5-HT2A |
260 |
Human |
[46]
|
5-HT2C |
780 |
Human |
[46]
|
α1B |
1,300 |
Human |
[46]
|
α2A |
2,900 |
Human |
[46]
|
α2B |
1,600 |
Human |
[46]
|
α2C |
2,100 |
Human |
[46]
|
D2 |
20,000 |
Rat |
[47]
|
H1 |
9.6–16 |
Human |
[48][46][46]
|
H2 |
>100,000 |
Canine |
[49]
|
H3 |
>10,000 |
Human |
[46][50][51]
|
H4 |
>10,000 |
Human |
[51]
|
M1 |
80–100 |
Human |
[52][46]
|
M2 |
120–490 |
Human |
[52][46]
|
M3 |
84–229 |
Human |
[52][46]
|
M4 |
53–112 |
Human |
[52][46]
|
M5 |
30–260 |
Human |
[52][46]
|
VGSC |
48,000–86,000 |
Rat |
[53]
|
hERG |
27,100 (IC50) |
Human |
[54]
|
Values are Ki (nM), unless otherwise noted. The smaller the value, the more strongly the drug binds to the site.
| |
Seroquel/Quetiapine (and metabolite)[46][47]
Site |
QTP |
NQTP |
Action |
Ref
|
SERT |
>10,000 |
927 |
Blocker |
[47]
|
NET |
>10,000 |
58 |
Blocker |
[47]
|
DAT |
>10,000 |
>10,000 |
ND |
[47]
|
5-HT1A |
320–432 |
45 |
Partial agonist |
[47][48]
|
5-HT1B |
1,109–2,050 |
1,117 |
ND |
[47][48]
|
5-HT1D |
>10,000 |
249 |
ND |
[47][48]
|
5-HT1E |
1,250–2,402 |
97 |
ND |
[47][48]
|
5-HT1F |
2,240 |
ND |
ND |
[48]
|
5-HT2A |
96–101 |
48 |
Antagonist |
[47][48]
|
5-HT2B |
ND |
14 |
Antagonist |
[47]
|
5-HT2C |
2,502 |
107 |
Antagonist |
[47]
|
5-HT3 |
>10,000 |
394 |
Antagonist |
[47]
|
5-HT4 |
ND |
ND |
ND |
ND
|
5-HT5A |
3,120 |
768 |
ND |
[47]
|
5-HT6 |
1,865 |
503 |
Antagonist |
[47]
|
5-HT7 |
307 |
76 |
Antagonist |
[47]
|
α1A |
22 |
144 |
Antagonist |
[47]
|
α1B |
39 |
95 |
Antagonist |
[47]
|
α2A |
2,230–3,630 |
237 |
Antagonist |
[47][48]
|
α2B |
90–747 |
378 |
Antagonist |
[47][48]
|
α2C |
28.7–350 |
736 |
Antagonist |
[47][48]
|
β1 |
>10,000 |
>10,000 |
ND |
[47][48]
|
β2 |
>10,000 |
>10,000 |
ND |
[47][48]
|
D1 |
712 |
214 |
Antagonist |
[47]
|
D2 |
245 |
196 |
Antagonist |
[47]
|
D2L |
700 |
ND |
Antagonist |
[48]
|
D2S |
390 |
ND |
Antagonist |
[48]
|
D3 |
340–483 |
567 |
Antagonist |
[47][48]
|
D4 |
1,202 |
1,297 |
Antagonist |
[47]
|
D4.2 |
1,600 |
ND |
Antagonist |
[48]
|
D5 |
1,738 |
1,419 |
Antagonist |
[47]
|
H1 |
2.2–11 |
3.5 |
Antagonist |
[47][48]
|
H2 |
>10,000 |
298 |
Antagonist |
[47]
|
H3 |
>10,000 |
>10,000 |
ND |
[47]
|
H4 |
>10,000 |
1,660 |
ND |
[47]
|
M1 |
858 |
39 |
Antagonist |
[47]
|
M2 |
1,339 |
453 |
ND |
[47]
|
M3 |
>10,000 |
23 |
Antagonist |
[47]
|
M4 |
542 |
110 |
ND |
[47]
|
M5 |
1,942 |
23 |
Antagonist |
[47]
|
σ1 |
220–3,651 |
>10,000 |
ND |
[47][48]
|
σ2 |
1,344 |
1,050 |
ND |
[47]
|
NMDA (PCP) |
>10,000 |
ND |
Antagonist |
[47]
|
VDCC |
>10,000 |
ND |
ND |
[47][48]
|
hERG |
ND |
>10,000 (IC50) |
ND |
[47]
|
Values are Ki (nM), unless otherwise noted. The smaller the value, the more strongly the drug binds to the site. All data are for human cloned proteins, except σ1 (guinea pig), σ2 (rat), and VDCC (rat).[47][48]
| |
Latuda/Lurasidone ()
|
Geodon/Ziprasidone
Ziprasidone[24]
Site |
Ki (nM) |
Action |
Ref
|
SERT |
112 |
Blocker |
[24]
|
NET |
44 |
Blocker |
[24]
|
DAT |
>10,000 |
ND |
[24]
|
5-HT1A |
2.5–76 |
Partial agonist |
[25][26][27]
|
5-HT1B |
0.99–4.0 |
Partial agonist |
[26][24]
|
5-HT1D |
5.1–9.0 |
Partial agonist |
[26][24]
|
5-HT1E |
360–1,279 |
ND |
[26][24]
|
5-HT2A |
0.08–1.4 |
Antagonist |
[28][25][26]
|
5-HT2B |
27.2 |
Antagonist |
[24]
|
5-HT2C |
0.72–13 |
Partial agonist |
[25]
|
5-HT3 |
>10,000 |
ND |
[24]
|
5-HT5A |
291 |
ND |
[24]
|
5-HT6 |
61–76 |
Antagonist |
[27][25]
|
5-HT7 |
6.0–9.3 |
Antagonist |
[24][27][25]
|
α1A |
18 |
Antagonist |
[24][27]
|
α1B |
9.0 |
Antagonist |
[24]
|
α2A |
160 |
Antagonist |
[24][26][27]
|
α2B |
48 |
Antagonist |
[24][26][27]
|
α2C |
59–77 |
Antagonist |
[24][26][27]
|
β1 |
≥2,570 |
ND |
[26][24]
|
β2 |
>10,000 |
ND |
[26][24]
|
D1 |
30–130 |
ND |
[24][25]
|
D2 |
4.8 |
Antagonist |
[29][25][27]
|
D2L |
4.6 |
Antagonist |
[26][30]
|
D2S |
4.2 |
Antagonist |
[26]
|
D3 |
7.2 |
Antagonist |
[29][25][26]
|
D4 |
0.8–105 |
Antagonist |
[29][25][24]
|
D4.2 |
28–39 |
Antagonist |
[30]
|
D4.4 |
14.9 |
Antagonist |
[31]
|
D5 |
152 |
ND |
[24]
|
H1 |
15–130 |
Antagonist |
[26][25][24]
|
H2 |
3,500 |
ND |
[24]
|
H3 |
>10,000 |
ND |
[24]
|
H4 |
>10,000 |
ND |
[24]
|
M1 |
≥300 |
ND |
[32][24][25]
|
M2 |
≥3,000 |
ND |
[32][24]
|
M3 |
≥1,300 |
ND |
[32][27][24]
|
M4 |
≥1,600 |
ND |
[32][24]
|
M5 |
≥1,600 |
ND |
[32][24]
|
σ1 |
110 |
ND |
[26]
|
σ2 |
ND |
ND |
ND
|
Opioid |
>1,000 |
ND |
[26]
|
nACh |
>10,000 |
ND |
[24]
|
NMDA (PCP) |
>10,000 |
ND |
[24]
|
VDCC |
>10,000 |
ND |
[24][26]
|
VGSC |
2,620 |
ND |
[26]
|
hERG |
169 |
Blocker |
[33]
|
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. All data are for human cloned proteins, except H3 (guinea pig), σ1 (guinea pig), opioid (rodent), NMDA/PCP (rat), VDCC, and VGSC.[24]
|
|
Asenapine/Saphris
Asenapine[12][6]
5-HT1A |
8.6 |
2.5 |
Partial agonist
|
5-HT1B |
8.4 |
4.0 |
Antagonist
|
5-HT2A |
10.2 |
0.06 |
Antagonist
|
5-HT2B |
9.8 |
0.16 |
Antagonist
|
5-HT2C |
10.5 |
0.03 |
Antagonist
|
5-HT5A |
8.8 |
1.6 |
Antagonist
|
5-HT6 |
9.5 |
0.25 |
Antagonist
|
5-HT7 |
9.9 |
0.13 |
Antagonist
|
α1 |
8.9 |
1.2 |
Antagonist
|
α2A |
8.9 |
1.2 |
Antagonist
|
α2B |
9.5 |
0.32 |
Antagonist
|
α2C |
8.9 |
1.2 |
Antagonist
|
D1 |
8.9 |
1.4 |
Antagonist
|
D2 |
8.9 |
1.3 |
Antagonist
|
D3 |
9.4 |
0.42 |
Antagonist
|
D4 |
9.0 |
1.1 |
Antagonist
|
H1 |
9.0 |
1.0 |
Antagonist
|
H2 |
8.2 |
6.2 |
Antagonist
|
mACh |
<5 |
8128 |
Antagonist
|
|
Solian |
|
|