DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

Table 16–2
Potencies of Antipsychotic Agents at Neurotransmitter Receptors a
DOPAMINE SEROTONIN 5HT 2A
/D 2
DOPAMINE MUSCARINIC ADRENERGIC HISTAMINE
D 2
5-HT 1A
5-HT 2A
5-HT 2C
RATIO D 1
D 4
M 1
α 1A
α 2A
H 1
Typical Agents
Haloperidol 1.2 2100 57 4500 47 120 5.5 >10,000 12 1130 1700
Fluphenazine 0.8 1000 3.2 990 3.9 17 29 1100 6.5 310 14
Thiothixene 0.7 410 50 1360 72 51 410 >10,000 12 80 8
Perphenazine 0.8 420 5.6 130 7.4 37 40 1500 10 810 8.0
Loxapine 11 2550 4.4 13 0.4 54 8.1 120 42 150 4.9
Molindone 20 3800 >5000 10,000 >250 >10,000 >2000 >10,000 2600 1100 2130
Thioridazine 8.0 140 28 53 3.5 94 6.4 13 3.2 130 16
Chlorpromazine 3.6 2120 3.6 16 1 76 12 32 0.3 250 3.1
Atypical Agents
Asenapine b 1.4 2.7 0.1 0.03 0.05 1.4 1.1 >10,000 1.2 1.2 1.0
Ziprasidone 6.8 12 0.6 13 0.1 30 39 >10,000 18 160 63
Sertindole b 2.7 280 0.4 0.90 0.2 12 13 >5000 1.8 640 130
Zotepine b 8.0 470 2.7 3.2 0.3 71 39 330 6.0 210 3.2
Risperidone 3.2 420 0.2 50 0.05 240 7.3 >10,000 5.0 16 20
Paliperidone 4.2 20 0.7 48 0.2 41 54 >10,000 2.5 4.7 19
Iloperidone 6.3 90 5.6 43 0.9 130 25 4900 0.3 160 12
Aripiprazole 1.6 6.0 8.7 22 5.0 1200 510 6800 26 74 28
Sulpiride b 6.4 >10,000 >10,000 >10,000 >1000 >10,000 54 >10,000 >10000 >5000 >10,000
Olanzapine 31 2300 3.7 10 0.1 70 18 2.5 110 310 2.2
Quetiapine 380 390 640 1840 2.0 990 2020 37 22 2900 6.9
Clozapine 160 120 5.4 9.4 0.03 270 24 6.2 1.6 90 1.1
a
Data are averaged K i
values (nM) from published sources determined by competition with radioligands for binding to the indicated cloned human receptors. Data derived from receptor binding
to human or rat brain tissue is used when cloned human receptor data is lacking.
b
Not available in the U.S.
Source: NIMH Psychoactive Drug Screening Program (PDSP) K i
Database: http://pdsp.med.unc.edu/pdsp.php (Accessed June 30, 2009).
CHAPTER 16
PHARMACOTHERAPY OF PSYCHOSIS AND MANIA
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