Aripiprazol

Aripiprazol

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 5-HT3 (rat), D4 (human/rat), H3 (guinea pig), and NMDA/PCP (rat). Percentages is for Intrinsic Activity.

5-HT1E
3000 - >10000 Ki (nM)
?

5-HT2A
6.7 - 39 Ki (nM)
12.7%
Very Weak Partial Agonist or Antagonist

5-HT2B
0.25 - 0.47 Ki (nM)
Inverse Agonist

5-HT2C
11 - 197 Ki (nM)
82%
Partial Agonist

5-HT3
520 - 740 Ki (nM)
?

5-HT5A
960 - 1520 Ki (nM)
87%
Near-Full Agonist

5-HT6
475 - 665 Ki (nM)
Antagonist

5-HT7
6.6 - 14 Ki (nM)
58%
Partial Agonist

α1A
26 Ki (nM)
Antagonist

α1B
35 Ki (nM)
Antagonist

α2A
74.3 Ki (nM)
Antagonist

α2B
102 Ki (nM)
?

α2C
38 Ki (nM)
Antagonist

β1
141 Ki (nM)
Antagonist

β2
163 Ki (nM)
Antagonist

D1
1290 - 2630 Ki (nM)
Partial Agonist

D2S
2.2 - 4.4 Ki (nM)
~60%
Partial Agonist

D2L
0.65 - 0.83 Ki (nM)
~50%
Partial Agonist

D3
4.3 - 15.1 Ki (nM)
~30%
Partial Agonist

D4
417 - 603 Ki (nM)
~30%
Partial Agonist

D5
1240 - 3940 Ki (nM)
Antagonist

H1
22.5 - 27.7 Ki (nM)
Neutral Antagonist

H2
>10000 Ki (nM)
?

H3
60 - 388 Ki (nM)
?

H4
>10000 Ki (nM)
?

M1
6780 Ki (nM)
?

M2
3510 Ki (nM)
?

M3
4680 Ki (nM)
?

M4
1520 Ki (nM)
?

M5
2330 Ki (nM)
?

GABAA-rho (GABAC)
?
Orthostatic Negative Allosteric Modulator

NMDA (PCP1)
1824 Ki (nM)
Uncompetitive Channel Blocker, Antagonist

NMDA (PCP2)
1824 Ki (nM)
Uncompetitive Agonist

SERT	900 - 1260 Ki (nM)	Reuptake Inhibitor
NET	1340 - 2840 Ki (nM)	Reuptake Inhibitor
DAT	2560 - 3880 Ki (nM)	Reuptake Inhibitor
5-HT1A	1.7 - 6.4 Ki (nM)	~68%	Partial Agonist
5-HT1B	570 - 1090 Ki (nM)	?
5-HT1D	57 - 79 Ki (nM)	?
PLACEHOLDER	PLACEHOLDER	PLACEHOLDER
PLACEHOLDER	PLACEHOLDER	PLACEHOLDER