规格: | 98% |
分子量: | 454.9 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
Background:
Prochlorperazine-d8is intended for use as an internal standard for the quantification of prochlorperazine by GC- or LC-MS. Prochlorperazine is a dopamine D2receptor antagonist with Kivalues of 4.7 and 2.9 nM for rat recombinant D2receptors in CHO cells and rat striatal membranes, respectively.1,2It also binds to rat recombinant D3receptors expressed in CHO cells (Ki= 35 nM) and to the serotonin (5-HT) receptor subtype 5-HT3in N1E-115 mouse neuroblastoma cell membranes (Ki= 1,200 nM).1,3Prochlorperazine (2 mg/kg) increases the latency to paw licking in a hot plate test, indicating analgesia, an effect that is blocked by antisense oligonucleotides against the M1muscarinic receptor.4It also inhibits emesis induced by apomorphine in dogs (ED50= 0.34 mg/kg).5Formulations containing prochlorperazine have been used in the treatment of psychotic disorders and as antiemetics.
1.Sokoloff, P., Giros, B., Martres, M.P., et al.Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neurolepticsNature137(6289)146-151(1990) 2.Tsuchihashi, H., Sasaki, T., Kojima, S., et al.Binding of [3H]haloperidol to dopamine D2 receptors in the rat striatumJ. Pharm. Pharmacol.44(11)911-914(1992) 3.Lummis, S.C., and Baker, J.Radioligand binding and photoaffinity labelling studies show a direct interaction of phenothiazines at 5-HT3 receptorsNeuropharmacology36(4-5)665-670(1997) 4.Ghelardini, C., Galeotti, N., Uslenghi, C., et al.Prochlorperazine induces central antinociception mediated by the muscarinic systemPharmacol. Res.50(3)351-358(2004) 5.Niemegeers, C.J.E.Antiemetic specificity of dopamine antagonistsPsychopharmacology (Berl).78(3)210-213(1982)