Summary of antagonist properties of S33138 at hD3, hD2L, and hD2S receptors as determined by blockade of DA-stimulated [35S]GTPγS binding, Gαi3 recruitment, and extracellular-regulated-kinase (ERK) phosphorylation
Data (pKi and pKB values) are means ± S.E.M. of three to four independent experiments.
hD3 | ||||||||||||||||||
| [3H]Spiperone | [35S]GTPγS | SPA (Gαi3) | ERK1/2 | |||||||||||||||
| pKi | pKB | % MOI | pKB | % MOI | pKB | % MOI |
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| 8.68 ± 0.01 | 8.85 ± 0.10 | 97 ± 3 | 8.24 ± 0.07 | 95 ± 7 | 9.08 ± 0.02 | 104 ± 4 |
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| hD2L | hD2S | |||||||||||||||||
| [3H]Spiperone | [35S]GTPγS | SPA (Gαi3) | ERK1/2 | [3H]Spiperone | [35S]GTPγS | |||||||||||||
| pKi | pKB | % MOI | pKB | % MOI | pKB | % MOI | pKi | pKB | % MOI | |||||||||
| 7.13 ± 0.03 | 7.82 ± 0.03 | 104 ± 8 | 7.76 ± 0.14 | 83 ± 12 | 8.03 ± 0.02 | 101 ± 2 | 7.26 ± 0.08 | 7.79 ± 0.06 | 96 ± 5 | |||||||||
MOI, maximal observed inhibition.