LP-211 is a brain penetrant selective agonist for a 5-HT7 receptor (Ki: 0.58 nM), and >300-fold selectivity over the 5-HT1A receptor.

D2 receptor:142 nM (Ki), 5-HT1A receptor:188 nM (Ki), 5-HT7 receptor:0.58 nM (Ki)

LP-211展示出高度亲和5-HT 7受体（Ki = 0.58 nM），对5-HT 1A和D 2受体具有高选择性（分别为324倍和245倍），并具有激动剂属性（最大效应=82%，EC 50 = 0.60 microM）[1]。LP-211的预处理对Fos样免疫活性无影响，但显著增强了辣椒素产生的反应[2]。

小鼠腹腔注射LP-211（10 mg/kg）后，该化合物迅速进入全身循环并进入大脑。其大脑浓度-时间曲线与血浆中的相似[1]。脊髓损伤（SCI）大鼠对LP-211（0.003-0.3 mg/kg, 静脉注射）的反应表现为剂量依赖性地增加膀胱容量和残余容量[3]。LP-211降低了第5层锥体神经元的突触整合，这在神经病理性疼痛中由于树突上的超极化激活和环核苷酸调节（HCN）通道功能失调而增强[4]。

Human 5-HT1A serotonin receptors stably expressed in HEK293 cells were radiolabeled with 1.0 nM [3H]-8-OH-DPAT. Samples containing 40 μg of membrane protein and different concentrations of each compound ranging from 0.1 nM to 10 μM were incubated in a final volume of 500 μL of 50 mM Tris-HCl pH 7.4, 5 mM MgSO4 for 120 min at 37 °C. After this incubation time, samples were filtered through GF/C presoaked in polyethylenimine 0.5% for at least 30 min prior to use. The filters were washed twice with 1 mL of ice-cold buffer (50 mM Tris-HCl, pH 7.4). Nonspecific binding was determined in the presence of 10 μM 5-HT [1].

Mice were given the test compounds intraperitoneally (10 mg/kg) and were killed by decapitation at various times thereafter. Mixed arteriovenous trunk blood was collected in heparinized tubes, centrifuged at 3000g for 10 min, and the plasma was stored at -20 °C. Brain was removed immediately, blotted with paper to remove surface blood, and quickly frozen in dry ice. Compounds and their 1-arylpiperazine metabolites were extracted from plasma and brain homogenate and quantified by reversed-phase HPLC with UV detection (230 nm). Briefly: to 0.1 mL of plasma, 0.2 mL of 20 mM of ammonium bicarbonate and 0.02 mL of a methanolic solution of the internal standard (100 μg/mL) were added; samples were then extracted twice with 1.5 mL of hexane containing 1% of isoamyl alcohol, and the combined extracts were evaporated to dryness and reconstituted in 0.15 mL of the mobile phase, which was injected into the chromatographic column. Brain tissue was homogenized in distilled water (1 g/10 mL), and 1 mL of the homogenate was extracted twice with 1.5 mL of hexane/isoamyl alcohol as described for plasma. Then, the organic phase was shaken with 0.2 mL of the mobile phase (LP-211 only); after centrifugation, 0.1 mL of the aqueous phase was injected into the chromatographic column [1].