Ro60-0175

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).¹ 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). ² 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 .³

1.Porter, R.H.P., Benwell, K.R., Lamb, H., et al.Functional characterization of agonists at recombinant human 5-HT2A, 5-HT2B and 5-HT2C receptors in CHO-K1 cellsBr. J. Pharmacol.128(1)13-20(1999) 2.Martin, J.R., B?s, M., Jenck, F., et al.5-HT2C receptor agonists: Pharmacological characteristics and therapeutic potentialJ. Pharmacol. Exp. Ther.286(2)913-924(1998) 3.Damjanoska, K.J., Muma, N.A., Zhang, Y., et al.Neuroendocrine evidence that (S)-2-(chloro-5-fluoro-indol-l-yl)-1-methylethylamine fumarate (Ro 60-0175) is not a selective 5-hydroxytryptamine2C receptor agonistJ. Pharmacol. Exp. Ther.304(3)1209-1216(2003)