LP-211

LP-211 is a brain-penetrant, selective **serotonin 5-HT7 receptor agonist** with high potency and selectivity. It exhibits a Ki value of **0.58 nM** at rat cloned 5-HT7 receptors and demonstrates over **300-fold selectivity** over the 5-HT1A receptor[1][3]. The compound functions as a **full agonist** at the 5-HT7 receptor, showing 82% maximal activity compared to 5-CT with an EC50 value of 0.60 μM[1]. LP-211 undergoes metabolic N-dealkylation to form **RA-7** (1-(2-diphenyl)piperazine), an active metabolite that concentrates in the brain and possesses even higher 5-HT7 receptor affinity (Ki = 1.4 nM) than the parent compound[1]. The compound has been developed as a research tool for investigating 5-HT7 receptor function and has demonstrated effects on body temperature regulation, novelty preference, and risk-prone behavior in preclinical studies. LP-211 was synthesized at the **Dipartimento Farmaco-Chimico, Università degli Studi di Bari**[1].

Other names

N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide