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(+)-PD 128907 hydrochloride

CAS No. : 300576-59-4

MCE 站：(+)-PD 128907 hydrochloride

产品活性：(+)-PD 128907 hydrochloride 是多巴胺D₂/D₃ 受体的选择性激动剂，其在人类和大鼠中对D₃ 的 K_i 值分别为0.7，0.84 nM，对D₂ 的K_i 值分别为179，770 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Dopamine Receptor

In Vitro: (+)-PD 128907 displaced [³H]spiperone binding from dopamine D₃ receptors (K_i human=1.7 nM and rat=0.84 nM) with >100-fold and 900-fold selectivity over the human (K_i=179 nM) and rat (K_i=770 nM) dopamine D₂ receptor.

In Vivo: (+)-PD 128907 significantly decreases dialysate DA levels in D₃ knock out mice. The IC₂₅ values are 61 nM and 1327 nM, respectively, for wild type and D₃knock out mice. The ratio of the IC₂₅ values shows that (+)-PD 128907 is 22 times more potent in decreasing dialysate DA levels in wild type as compared to mice lacking the D₃ receptor. The D3 agonist evokes a dose related decrease in dialysate DA in wild type mice. Post-hoc analysis shows that all doses tested (0.03, 0.1 and 0.3 mg/kg) significantly inhibit dialysate DA. The IC₂₅ values are 0.05 and 0.44 mg/kg for wild type and knock out mice, respectively, indicating that systemically administered (+)-PD 128907 is 9 times more potent in decreasing dialysate DA in the ventral striatum of wild type as compared to D₃ knock out mice. Doses of 1 mg/kg or higher of (+)-PD 128907 markedly inhibits dialysate DA in both wild type and D₃ knock out mice.

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