adoprazine
adoprazine Basic information
- Product Name:
- adoprazine
- Synonyms:
-
- adoprazine
- 1-(2,3-Dihydro-1,4-benzodioxin-5-yl)-4-[[5-(4-fluorophenyl)-3-pyridinyl]methyl]piperazine
- Unii-7snb18Q89d
- SLV 313
- SLV313
- Adoprazine (SLV313)
- SLV 313;SLV313;SLV-313
- Piperazine, 1-(2,3-dihydro-1,4-benzodioxin-5-yl)-4-[[5-(4-fluorophenyl)-3-pyridinyl]methyl]-
- CAS:
- 222551-17-9
- MF:
- C24H24FN3O2
- MW:
- 405.46
- Mol File:
- 222551-17-9.mol
adoprazine Chemical Properties
- Boiling point:
- 565.0±50.0 °C(Predicted)
- Density
- 1.256
- storage temp.
- Store at -20°C
- solubility
- DMSO : 50 mg/mL (123.32 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
- form
- Powder
- pka
- 6.07±0.10(Predicted)
- color
- Light yellow to yellow
adoprazine Usage And Synthesis
Uses
Adoprazine (SLV313) is a full 5-HT1A receptor agonist with a pEC50 of 9 at cloned h5-HT1A receptors. Adoprazine (SLV313) is a full D2 and D3 receptor antagonist with pA2s of 9.3 and 8.9 at hD2 and hD3 receptors, respectively. Adoprazine (SLV313) has the characteristics of atypical antipsychotics[1].
Biological Activity
Adoprazine (SLV313) is a full agonist at the 5-HT1A receptor with a pEC50 of 9 at the h5-HT1A receptor. Adoprazine (SLV313) is a complete antagonist of D2 and D3 receptors with a pA2 value of 9.3 in hD2 receptor and 8.9 in hD3 receptor. It (SLV313) has atypical antipsychotic properties.
in vitro
Adoprazine (SLV313) has high affinity at human recombinant D 2 , D 3 , D 4 , 5-HT < sub> 2B , and 5-HT 1A receptors, with pK i s of 8.4, 8.4, 8.0, 7.9 and 9.1 , respectively. Adoprazine (SLV313) acts as a high potency dopamine D 2 receptor antagonist and an efficacious serotonin 5-HT 1A receptor agonist, with E max value (% effect of 10 μM 5-HT) of 73 and pK B value of 8.5 .
in vivo
Adoprazine (SLV313) (0.1-10 mg/kg; po; single) is sufficient to reduce extracellular 5-HT and increase dopamine levels in the nucleus accumbens in a dose- and time-dependent manner.
| Animal Model: | Male Wistar rats (275-350 g) |
| Dosage: | 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg |
| Administration: | po; single |
| Result : | Led to a dose- and time-dependent increase in extracellular levels of DA, DOPAC, and HVA. In contrast, led to a reduction in 5-HT levels and no change in 5-HIAA levels. |
target
| 5-HT 1A Receptor 9 (pEC 50 ) | D 2 < /sub> Receptor 9.3 (pA2) | D 3 Receptor 8.9 (pA2) | D 4 Receptor 8.0 (pKi) | 5-HT 7 Receptor 7.2 (pKi) | 5-HT 1A < /sub> Receptor 9.1 (pKi) | D 2 Receptor 8.4 (pKi) | D 3 Receptor 8.4 (pKi) |
IC 50
5-HT1A Receptor: 9 (pEC50); D2 Receptor: 9.3 (pA2); D3 Receptor: 8.9 (pA2); D4 Receptor: 8.0 (pKi); 5-HT7 Receptor: 7.2 (pKi); 5-HT1A Receptor: 9.1 (pKi); D2 Receptor: 8.4 (pKi); D3 Receptor: 8.4 (pKi)
References
[1] Andrew C McCreary, et al. SLV313 (1-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-4- [5-(4-fluoro-phenyl)-pyridin-3-ylmethyl]-piperazine monohydrochloride): a novel dopamine D2 receptor antagonist and 5-HT1A receptor agonist potential antipsychotic drug. Neuropsychopharmacology. 2007 Jan;32(1):78-94. DOI:10.1038/sj.npp.1301098
[2] Liesbeth A Bruins Slot, et al. Differential profile of antipsychotics at serotonin 5-HT1A and dopamine D2S receptors coupled to extracellular signal-regulated kinase. Eur J Pharmacol. 2006 Mar 18;534(1-3):63-70. DOI:10.1016/j.ejphar.2006.01.027
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