LP-211

SKU: orb1301833

Description

LP-211 is a potent and selective 5-HT7 receptor agonist with high brain penetrance, exhibiting a Ki of 0.58 nM and over 300-fold selectivity versus the 5-HT1A receptor. This tool compound is widely used in neuroscience research to investigate the receptor's role in circadian rhythms, learning, and mood, utilizing both in vitro binding assays and in vivo behavioral models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1052147-86-0
• MW: 466.62
• Purity: 99.7%
• Formula: C₃₀H₃₄N₄O
• SMILES: C(CCCCC(NCC1=CC=C(C#N)C=C1)=O)N2CCN(C3=C(C=CC=C3)C4=CC=CC=C4)CC2
• Target: Dopamine Receptor,5-HT Receptor
• Solubility: DMSO:90 mg/mL (192.88 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.07 mM)

Bioactivity

• Target IC50:
  5-HT7 receptor:0.58 nM (Ki)|5-HT1A receptor:188 nM (Ki)|D2 receptor:142 nM (Ki)
• In Vivo:
  After intraperitoneal injection in mice, LP-211 (10 mg/kg) rapidly reached the systemic circulation and entered the brain. Its brain concentration-time profile paralleled that in plasma . SCI rats responded to LP-211 (0.003-0.3, mg/kg, i.v.) with dose-dependent increases in bladder capacity and residual volume . LP-211 reduced synaptic integration in layer 5 pyramidal neurons, which was enhanced in neuropathic pain due to a dysfunction of dendritic hyperpolarization-activated-and-cyclic-nucleotide-regulated (HCN) channels .
• In Vitro:
  LP-211 showed high 5-HT 7 receptor affinity (Ki = 0.58 nM), high selectivity over 5-HT 1A and D 2 receptors (324- and 245-fold, respectively), and agonist properties (maximal effect = 82%, EC 50 = 0.60 microM) . Pretreatment with LP-211 had no effect on Fos-like immunoreactivity but strongly increased the response produced by capsaicin .
• Animal Research:
  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 .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5-HT7, 5HT Receptor, 5HTReceptor, 5-hydroxytryptamine Receptor, 5-HT1A, 5-HT Receptor, D2, Dopamine Receptor, DopamineReceptor, inhibit, Inhibitor, LP 211, LP211, LP-211, Serotonin Receptor

Compound Identifiers

PubChem CID

25107716