Which drug is a partial agonist at D2 and D3 with high 5-HT1A affinity and is associated with D3 receptor activity?

Which drug is a partial agonist at D2 and D3 with high 5-HT1A affinity and is associated with D3 receptor activity?

• A. Aripiprazole
• B. Brexpiprazole
• C. Cariprazine
• D. Ziprasidone

Answer: (C)

Dopamine D2 and D3 partial agonism with strong D3 affinity and 5-HT1A activity defines a drug profile aimed at balancing positive symptoms while offering potential improvements in negative symptoms and cognition. Cariprazine fits this profile best because it preferentially binds to the D3 receptor and acts as a partial agonist there, while also acting as a partial agonist at D2 and engaging 5-HT1A receptors. This D3-heavy activity is associated with the clinical benefits seen on negative symptoms and functioning, setting it apart from other agents that also target D2 and 5-HT1A but lack strong D3 selectivity. Aripiprazole and brexpiprazole have D2 partial agonism and 5-HT1A activity but do not emphasize D3 as much, and ziprasidone is mainly a D2/D3 antagonist with different receptor targets overall, not a D3 partial agonist.

Dopamine D2 and D3 partial agonism with strong D3 affinity and 5-HT1A activity defines a drug profile aimed at balancing positive symptoms while offering potential improvements in negative symptoms and cognition. Cariprazine fits this profile best because it preferentially binds to the D3 receptor and acts as a partial agonist there, while also acting as a partial agonist at D2 and engaging 5-HT1A receptors. This D3-heavy activity is associated with the clinical benefits seen on negative symptoms and functioning, setting it apart from other agents that also target D2 and 5-HT1A but lack strong D3 selectivity. Aripiprazole and brexpiprazole have D2 partial agonism and 5-HT1A activity but do not emphasize D3 as much, and ziprasidone is mainly a D2/D3 antagonist with different receptor targets overall, not a D3 partial agonist.