adoprazine

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

in vivo

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-HT_1A 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-HT_1A 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