PD 119819
PD 119819 Basic information
- Product Name:
- PD 119819
- Synonyms:
-
- PD 119819
- 7-<3-<4-(2-pyridinyl)-1-piperazinyl>propoxy>-4H-1-benzopyran-4-one dihydrochloride
- PD119819' PD-119819
- CAS:
- 105277-43-8
- MF:
- C21H24ClN3O3
- MW:
- 401.89
- Mol File:
- 105277-43-8.mol
PD 119819 Usage And Synthesis
Description
PD 119819 is a heterocyclic piperazine and has been identified as an extremely selective DA autoreceptor agonist in tests that include [3H]haloperidol binding, inhibition of spontaneous locomotor activity, inhibition of brain DA synthesis, inhibition of brain DA neuronal firing, stereotypy assessment, and reversal of 6-hydroxydopamine (6-OHDA) induced akinesia in rats.
Uses
PD 119819 is a highly selective benzopyran-4-one brain dopamine autoreceptor agonist. PD 119819, a heterocyclic piperazine, inhibits spontaneous locomotor activity and brain dopamine synthesis[1][2].
in vivo
PD 119819 (5~80 mg/kg; nasogastric intubation) makes monkeys show marked increases in alanine aminotransferase levels and a moderate increase in ornithine carbamyltransferase levels at the initial sampling interval after doses of 5 mg/kg with peak levels occurring after doses of 20 or 60 mg/kg, while lower values is evident after doses of 80 mg/kg[1].
| Animal Model: | Cynomolgus monkey[1] |
| Dosage: | 5~80 mg/kg |
| Administration: | Nasogastric intubation |
| Result: | Made monkeys show marked increases in alanine aminotransferase levels and a moderate increase in ornithine carbamyltransferase levels at the initial sampling interval after doses of 5 mg/kg with peak levels occurring after doses of 20 or 60 mg/kg, while lower values were evident after doses of 80 mg/kg. |
IC 50
Dopamine Receptor
References
[1] Macallum GE, et al. Renal and hepatic toxicity of a benzopyran-4-one in the Cynomolgus monkey. Toxicology. 1989;59(1):97-108. DOI:10.1016/0300-483x(89)90159-5
[2] Jaen JC, et al. Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones. J Med Chem. 1991;34(1):248-256. DOI:10.1021/jm00105a039