169675-09-6

Ro 60-0175 is an agonist of the serotonin (5-HT) receptor subtype 5-HT₂ that stimulates increases in intracellular calcium levels in CHO-K1 cells expressing human 5-HT_2A, 5-HT_2B, and 5-HT_2C receptors (EC₅₀s = 447, 0.9, and 32 nM, respectively). It is selective for human 5-HT_2A and 5-HT_2C (K_is = 32 and 1 nM, respectively) over human 5-HT_1A, 5-HT_1D, 5-HT₆, and 5-HT₇, rat 5-HT_1B and 5-HT₃, and guinea pig 5-HT₄ receptors (K_is = ≥1,995 nM), as well as adenosine A₁ and A₂, histamine H_1-3, dopamine D_1-5, α₁-, α₂-, and β₁-adrenergic, M_1-5 muscarinic, nicotinic, kainate, AMPA, and μ-, δ-, and κ-opioid receptors (IC₅₀s = >1,000 nM), but does bind to β₂-adrenergic receptors (IC₅₀ = 251 nM). In vivo, Ro 60-0175 increases plasma levels of corticosterone, oxytocin, and prolactin in rats (ED₅₀s = 2.43, 4.19, and 4.03 mg/kg, respectively), effects that are not inhibited by the 5-HT_2C antagonist SB-242084 or the 5-HT_2A antagonist MDL 100,907 (volinanserin; ).

Ro 60-0175 fumarate is a potent and selective SR-2 agonist.

Potent, selective 5-HT 2 receptor agonist; shows selectivity for the 5-HT 2C subtype (pK i values are 9, 7.5, 5.4, 5.2 and 5.6 for human 5-HT 2C , 2A , 1A , 6 and 7 receptors respectively). Centrally active following oral or systemic administration in vivo .

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