(+)-PD 128907 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

(+)-PD 128907 盐酸盐是 D3 多巴胺受体的激动剂。

(+)-PD 128907 hydrochloride is an agonist of D3 dopamine receptor .

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

(+)-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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GPCR/G Protein

Dopamine Receptor

Dopamine

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300576-59-4

285.77

C14H20ClNO3

>98% (HPLC)

DMSO:150 mg/mL (524.90 mM)

CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21.Cl

(4aS10bS)-4-Propyl-34a510b-tetrahydro-2H-chromeno[43-b][14]oxazin-9-ol Hydrochloride

(-20℃)

With Ice Pack

≥ 2 years