5-HT2A agonist (R)-69 is a potent selective 5-HT2A receptor partial agonist with EC50 of 41 nM in calcium flux assays, and Ki value of 680 nM.
(R)-69 has an agonist EC50 of 190 nM versus 5-HT2BR, 4.6-fold selective for the 5-HT2AR, and >30-fold selectivity over 5-HT2AC.
(R)-69 shows modest (0.8 μM) activity for the serotonin transporter SERT, is inactive versus the DAT or NET transporters.
(R)-69 does not possess locomotor-stimulating or reinforcing activity, exerts no effects on prepulse inhibition (PPI) relative to LSD.
(R)-69 demonstrates anxiolytic-like and strong antidepressant drug-like effects in mouse models.
