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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Neuronal Signal Pathway > LP-211CAS：1052147-86-0
Molecular Formula：C30H34N4O
Molecular Weight：466.62
Storage：Store at -20℃，2 years
Purity：≥98%
Appearance：Light yellow to yellow Oil
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| CAS | 1052147-86-0 |
| Name | LP-211 |
| Molecular Formula | C30H34N4O |
| Molecular Weight | 466.62 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Oil |
| Storage | Store at -20℃，2 years |
| SMILES | C1CN(CCN1CCCCCC(=O)NCC2=CC=C(C=C2)C#N)C3=CC=CC=C3C4=CC=CC=C4 |
| Target Point | 5-HT Receptor |
| Passage | Neuronal Signaling;GPCR & G Protein |
| Background | LP-211 is a selective and blood?brain barrier penetrant 5-HT7 receptor agonist， with a Ki of 0.58 nM， with high selectivity over 5-HT1A receptor (Ki， 188 nM) and D2 receptor (Ki， 142 nM).[1-3] |
| In Vivo | LP-211 is a selective 5-HT7 receptor agonist， with a Ki of 0.58 nM， 324- and 245-fold selectivity over 5-HT1A receptor (Ki， 188 nM) and D2 receptor (Ki， 142 nM). LP-211 shows agonist properties with an EC50 of 0.6 μM[1]. |
| Cell Experiment | LP-211 (10 mg/kg， i.p.) rapidly reaches the systemic circulation in the mouse， with mean Cmax of 0.76 ± 0.32 μg/mL at 30 min[1]. LP-211 (0.003-0.3 mg/kg， i.p.) significantly increases the micturition volume in a dose-dependent manner， and causes significant increases in voiding efficiency in spinal cord-injured (SCI) rats， and such effects can be completely reversed by SB-269970[2]. LP-211 (0.25 and 0.50 mg/kg i.p.) improves consolidation of chamber-shape memory in rats， resulting in significant novelty-induced hyperactivity and recognition[3]. |
| Kinase Experiment | Thirty male adult Wistar rats (300-450 g) are assessed for novelty preference behavior after acute treatment (administered immediately after the training session and 24 h before the test session). After a 4 weeks wash out， the rPDT is conducted to evaluate attraction from a greater/uncertain reward， with a sub-chronic treatment (five injections， immediately after sessions which follow the indifferent point). Food restriction， imposed by the experimenter through a limited quantity of food given at the end of each rPDT session， is applied to increase motivation to work for food delivery. All behavioral tests take place between 9:30 am and 4:00 pm. Rats are randomly assigned to treatment (LP-211 at 0.25 or 0.50 mg/kg i.p.) and control groups (injection volume 10 mL/kg; n?=?10 per group). The brain penetrant 5-HT7R agonist LP-211 is dissolved in a vehicle solution of 1% dimethyl sulfoxide (DMSO) in saline (0.9% NaCl). Control group receives the vehicle strictly in the same conditions[3]. |
| Data Literature Source | Binding of [3H]-LSD at rat cloned 5-HT7 receptor is performed in the assay. In 1 mL of incubation buffer (50 mM Tris， 10 mM MgCl2 and 0.5 mM EDTA， pH 7.4) are suspended 30 μg of membranes， 2.5 nM [3H]-LSD， LP-211 (6?9 concentrations). The samples are incubated for 60 min at 37°C. The incubation is stopped by rapid filtration on GF/A glass fiber filters (presoaked in 0.5% polyethylenimine for 30 min). The filters are washed with 3 × 53 mL of ice-cold buffer (50 mM Tris， pH 7.4). Nonspecific binding is determined in the presence of 10 μM 5-CT. Approximately 90% of specific binding is determined under these conditions[1]. |
| Unit | Bottle |
| Specification | 1mg 5mg 10mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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