LP-211
Catalog No.: GC30880Purity:>99.50%
LP-211 is a selective, blood-brain barrier-permeable 5-HT7 receptor agonist (Ki=0.58nM) with higher selectivity over the 5-HT1A receptor (Ki=188nM) and the D2 receptor (Ki=142nM).
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Cas No.: 1052147-86-0
10mM (in 1mL DMSO)In Stock
$58.00
1
1mgIn Stock
$25.00
1
5mgIn Stock
$56.00
1
10mgIn Stock
$87.00
1
25mgIn Stock
$171.00
1
50mgIn Stock
$273.00
1
100mgIn Stock
$419.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $58.00 | In Stock | 1 | |
| 1mg | $25.00 | In Stock | 1 | |
| 5mg | $56.00 | In Stock | 1 | |
| 10mg | $87.00 | In Stock | 1 | |
| 25mg | $171.00 | In Stock | 1 | |
| 50mg | $273.00 | In Stock | 1 | |
| 100mg | $419.00 | In Stock | 1 |
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Citations
1 publicationsPublications from researchers using this productDescription
LP-211 is a selective, blood-brain barrier-permeable 5-HT7 receptor agonist (Ki=0.58nM) with higher selectivity over the 5-HT1A receptor (Ki=188nM) and the D2 receptor (Ki=142nM)[1-2]. LP-211 can modulate histone H3 acetylation levels and influence the association of the MeCP2 co-repressor protein by activating the 5-HT7 receptor. LP-211 can be used in research related to neurodevelopmental disorders such as Rett syndrome and Fragile X syndrome, as well as neuropathic pain and memory impairment[3-4].
In vitro, LP-211 (10µM) stimulated THP-1-derived macrophages for 48 hours. LP-211 significantly reduced the phagocytic and migratory capacity of pro-inflammatory M1-like macrophages, while also altering the cytokine and chemokine secretion profiles of all macrophage types (M0, M1, M2a, M2c)[5]. LP-211 (1µM) was incubated with mitochondria purified from human SH-SY5Y neuroblastoma cells for 3 minutes. LP-211 did not significantly affect the activity of mitochondrial respiratory chain cytochrome c oxidas[6].
In vivo, a single intraperitoneal injection of LP-211 (3mg/kg) was administered to male Fmr1-KO (B6.129P2-Fmr1tm1Cgr/J) mice, 30 minutes prior to behavioral testing. LP-211 significantly reduced the duration of their self-grooming behavior[7]. Single intraperitoneal injection of LP-211 (10mg/kg) was administered to adult male C57BL/6 mice 7-10 days after chronic constriction injury (CCI) surgery. The effects began 30 minutes post-injection and peaked between 90-150 minutes. LP-211 significantly increased the mechanical withdrawal threshold of the injured hind paw and completely blocked the place preference shift induced by noxious stimulation in the place escape/avoidance paradigm[8].
References:
[1] Leopoldo M, Lacivita E, De Giorgio P, et al. Structural modifications of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides: influence on lipophilicity and 5-HT7 receptor activity. Part III. J Med Chem. 2008 Sep 25;51(18):5813-22.
[2] Beaudet G, Paizanis E, Zoratto F, et al. LP-211, a selective 5-HT7 receptor agonist, increases novelty-preference and promotes risk-prone behavior in rats. Synapse. 2017 Dec;71(12).
[3] Norouzi-Javidan A, Javanbakht J, Barati F, et al. Effect of 5-HT7 receptor agonist, LP-211, on micturition following spinal cord injury in male rats. Am J Transl Res. 2016 Jun 15;8(6):2525-33.
[4] Rahdar M, Davoudi S, Dehghan S, et al. Reversal of electrophysiological and behavioral deficits mediated by 5-HT7 receptor upregulation following LP-211 treatment in an autistic-like rat model induced by prenatal valproic acid exposure. Neuropharmacology. 2024 Oct 1;257:110057.
[5] Bahr FS, Müller FE, Kasten M, et al. Serotonin receptor 5-HT7 modulates inflammatory-associated functions of macrophages. Cell Mol Life Sci. 2025 Jan 21;82(1):51.
[6] Tempio A, Niso M, Laera L, et al. Mitochondrial Membranes of Human SH-SY5Y Neuroblastoma Cells Express Serotonin 5-HT7 Receptor. Int J Mol Sci. 2020 Dec 17;21(24):9629.
[7] Sharghi S, Flunkert S, Daurer M, et al. Evaluating the effect of R-Baclofen and LP-211 on autistic behavior of the BTBR and Fmr1-KO mouse models. Front Neurosci. 2023 Mar 30;17:1087788.
[8] Santello M, Bisco A, Nevian NE, et al. The brain-penetrant 5-HT7 receptor agonist LP-211 reduces the sensory and affective components of neuropathic pain. Neurobiol Dis. 2017 Oct;106:214-221.
Protocol
| Cell experiment [1]: | |
Cell lines | THP-1-derived macrophages and human CD14+ cell-derived macrophages |
Preparation Method | THP-1 monocytes were differentiated into macrophages (M0, M1-like, M2a-like, M2c-like) using PMA and specific polarizing agents. Human CD14+ cells from PBMCs were differentiated into M1-like and M2-like macrophages using GM-CSF and M-CSF, respectively. Macrophages were stimulated with LP-211 (10μM) starting on day 3 or day 5 after seeding. |
Reaction Conditions | 10μM; 48 hours. |
Applications | LP-211 significantly reduced the phagocytic and migratory ability of pro-inflammatory M1-like macrophages. LP-211 treatment led to changes in the secretory properties (cytokine and chemokine profiles) of all macrophage types (M0, M1, M2a, M2c), with the highest effects observed for M0- and M2c-like macrophages. The importance of 5-HT7R for regulating phagocytosis was confirmed in human primary CD14+ cell-derived M2-like macrophages. |
| Animal experiment [2]: | |
Animal models | Male BTBR T+ Itpr3tf/J mice and male B6.129P2-Fmr1tm1Cgr/J (Fmr1-KO) mice |
Preparation Method | Animals received an acute intraperitoneal injection of LP-211 30 minutes prior to a series of behavioral tests performed starting at 5 weeks of age. Tests included the open field test, elevated plus maze (EPM), and self-grooming test. |
Dosage form | 3mg/kg; i.p.; single injection per test session. |
Applications | Acute LP-211 administration did not affect the behavioral abnormalities (anxiety, repetitive behavior) observed in BTBR mice. In Fmr1-KO mice, acute LP-211 treatment significantly improved repetitive behavior by reducing self-grooming duration and showed a trend to change anxiety levels, as evidenced by a decreased frequency of entries into the open arms of the EPM. |
References: | |
Product Documents
Purity:>99.50%Appearance:A solid
Chemical Properties
CAS No.
1052147-86-0
SMILES
O=C(NCC1=CC=C(C#N)C=C1)CCCCCN2CCN(C3=CC=CC=C3C4=CC=CC=C4)CC2
Molecular Formula
C30H34N4O
Molecular Weight
466.62
Solubility
DMSO : ≥ 106.6 mg/mL (228.45 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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