Dopamine D1 receptors are important G protein-coupled receptors in the central nervous system (CNS). They activate different effectors through G protein coupling and interact with the neurotransmitter dopamine to signal. Dopamine receptors are matter to a variety of neural processes such as cognition, memory, learning, and fine motor control. Meanwhile, the effectiveness of dopamine (DA) D1 antagonism in suppressing Schizophrenia has been demonstrated. Adenylate cyclase (AC) activation conducts the primary function of dopamine D1 receptors. That is we’ll introduce a selective dopamine receptor agonist, SKF 83822.

SKF 83822 selectively activates the AC instead of the PLC.

Classical effectors of the dopamine D1 receptor include phosphoinositide (PI), adenylate cyclase (AC), and phospholipase C (PLC). SKF 83822 is able to specifically activate AC while promoting cAMP production to further stimulate AC activation. In in vivo studies, SKF 83822 (25-100 μg/kg; s.c.; single dose) following antagonist, produces a strong rotational response in rats in a dose-dependent manner. SKF 83822 (0.005-0.625 mg/kg, 2 mL/kg; s.c.; single dose) also induces mandibular vertical movement and incisor chatter in C57BL/6J mice. Moreover, SKF 83822 (0.15-0.35 mg/kg; subcutaneous injection; single dose) induces locomotion without inducing dyskinesias, without stereotyping.

However, compared with general dopamine D1 receptor agonists, SKF 83822 has special advantages. A number of dopamine D1 agonists stimulate PI signaling or interact with PLC but not AC. In contrast, SKF 83822 specifically activates AC but not PLC. rendering it unable to induce oral dyskinesias in prepared monkeys may have antiparkinsonian effects. SKF 83822 may also be less likely to induce dyskinesias and some other side effects.

Above all, SKF 83822 is a selective D1 receptor agonist targeting adenylate cyclase.


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