TABLE 2.
Effects of selected antipsychotics, D3R agonists, antagonists, on the [3H](+)-PHNO uptake in rat striatum and cerebellum L9,10 region*,&.
| Route | Administered highest dose (mg/kg) | Striatal ED50 (mg/kg) | CB L9/10 ED50 (mg/kg) | Striatum/ CB L9,10 ratio |
|
| Agonists | |||||
| (+)-PHNO | p.o. | 1 | >1 (33) | 0.05 (95) | >>20 |
| (−)-Pramipexole (PRP) | s.c. | 1 | >1 (39) | 0.018 (96) | >>55 |
| Partial agonists | |||||
| Aripiprazole (ARP) | p.o. | 30 | 7.65 (92) | >30 (14) | <<0.26 |
| Cariprazine (CAR) | p.o. | 3 | 0.23 (99) | 0.43 (99) | 0.53 |
| Cariprazine | i.v. | 0.023 (94) | 0.035 (98) | 0.66 | |
| DD-CAR+ | p.o. | 10 | 0.58 (99) | 0.41 (100) | 0.66 |
| Antagonists | |||||
| Amisulpride (AMS) | i.p. | 30 | >30 (35) | 3.0 (82) | >10 |
| Asenapine (ASN) | s.c. | 1 | 0.037 (95) | 0.177 (74) | 0.21 |
| Clozapine# (CLZ) | p.o. | 60 | 60 (34) | 60 (29) | n.c. |
| Haloperidol (HP) | p.o. | 3 | 0.23 (100) | 1.05 (100) | 0.22 |
| Olanzapine (OLZ) | p.o. | 30 | 1.46 (91) | ∼30 (48) | ∼0.05 |
| Quetiapine# QUET) | p.o. | 250 | 250 (36) | 250 (36) | n.c. |
| Raclopride (RCP) | s.c. | 1 | 0.013 (98) | 0.072 (97) | 0.18 |
| Risperidone (RSP) | p.o. | 3 | 0.29 (89) | ∼2.3 (53) | ∼0.13 |
| SB-277011A (SB) | p.o. | 30 | >30 (28) | 1.31 (100) | >>23 |
| SV-156 | s.c. | 10 | 0.89 (84) | >12 (20) | <<0.07 |
| Ziprasidone (ZPR) | p.o. | 30 | 1.63 (92) | ∼30 (52) | ∼0.05 |
*The ED50 doses were calculated from individual dose response curves consisting of at least 4–5 doses with 3–8 animals in each dose-group. Group means were analyzed by one-way analysis of variance (ANOVA) followed by Tukey-Kramer post-hoc multiple comparison test. The highest inhibition percentage achieved at the highest applied are given in the brackets. Where the highest achieved inhibition at highest applied dose was around 50% percent, approximate ED50 values are given and are marked with ∼ sign.
+DD-CAR, didesmethyl-cariprazine; one of the major human metabolites of cariprazine.
#In case of clozapine and quetiapine the highest achievable inhibition was less than 50%, thus ED50 could not be calculated.
&Kiss et al. (82).