1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor

Lorcaserin Hydrochloride (Synonyms: APD356)

Cat. No.: HY-15368 Purity: 99.95%
Data Sheet SDS Handling Instructions

Lorcaserin (Hydrochloride) is a selective full agonist of human 5-HT2C receptor with Ki of 15 nM.

For research use only. We do not sell to patients.
Lorcaserin Hydrochloride Chemical Structure

Lorcaserin Hydrochloride Chemical Structure

CAS No. : 846589-98-8

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10 mM * 1 mL in DMSO USD 66 In-stock
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10 mg USD 84 In-stock
50 mg USD 168 In-stock
100 mg USD 252 In-stock
200 mg USD 372 In-stock
500 mg USD 540 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Lorcaserin (Hydrochloride) is a selective full agonist of human 5-HT2C receptor with Ki of 15 nM.

IC50 & Target

Ki: 15 nM (5-HT2C)

In Vitro

Lorcaserin is 18-fold more potent at human 5-HT2C (EC50= 9 nM) than at human 5-HT2A (EC50= 168 nM), and it is 104-fold more potent at human 5-HT2C than human 5-HT2B (EC50= 943 nM)[1].

In Vivo

Lorcaserin decreases cumulative food intake at 2, 4, 6, and 22 h with a significant decrease continuing throughout the 22-h duration of the study at the highest dose (24 mg/kg) only. The reduction in food intake induced by lorcaserin (18 mg/kg, p.o.) is mediated by 5-HT2C and not 5-HT2A receptors. Lorcaserin significantly reduces active, and increased inactive counts, and increases the incidence of penile grooming, an effect mediated by the 5-HT2C receptor[1]. Lorcaserin (20 mg/kg) doses causes a significant linear dose-related reduction in responses on the active lever but has no significant effect on the response to the inactive lever. Lorcaserin (0.3125, 0.625, 1.25, and 2.5 mg/kg) also produces a significant reduction in nicotine self-administration[2].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 4.3076 mL 21.5378 mL 43.0756 mL
5 mM 0.8615 mL 4.3076 mL 8.6151 mL
10 mM 0.4308 mL 2.1538 mL 4.3076 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

For development of functional human and rat 5-HT2A, 5-HT2B, and 5-HT2C inositol accumulation assays, recombinant 5-HT2 receptors are transiently expressed in HEK293 cells using the Lipofectamine method. In brief, cells are incubated in 15-cm plates with DMEM, and they are grown to at least 60 to 80% confluence, rinsed with Opti-MEM I media, followed by addition of 2 mL of Opti-MEM I containing 60 μL of Lipofectamine and 16 μg of cDNA for human and rat 5-HT2A and 5-HT2B receptors or 15 μL of Lipofectamine and 16 μg of cDNA for human and rat 5-HT2C receptors. Cells are then incubated for 5 h at 37°C in a 5% CO2 incubator. Next, cells are aspirated, and 30 mL of DMEM is added. Cells are then used for assays 24 h after transfection. Under these conditions, cells expressing human 5-HT2C receptor display constitutive elevation of inositol phosphate accumulation that is reversed by the inverse agonist mianserin, whereas cells expressing human 5-HT2A and 5-HT2B receptors display considerably less constitutive activity. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Lorcaserin is formulated in deionized water.

Male Sprague-Dawley rats (250-300 g) are obtained from Harlan. On the day of the experiment, rats receives a single dose of lorcaserin in water via oral gavage. Dosing volume and dose are 5 mL/kg and 10 mg/kg, respectively. Lorcaserin is formulated in deionized water. The following sampling scheme is used (n=3/time point): 0.25, 0.5, 1, 2, 4, 8, 12, 24, and 40 h after dose. Rats are lightly anesthetized with isoflurane, blood is collected via cardiac puncture, and brains are removed from the cranium. Blood samples are dispensed into sodium-heparinized vials, and then vials are capped and stored at 4°C. Plasma is separated from formed elements in blood by centrifugation (10 min at 3000 g), and then plasma is frozen. Brains are rinsed with ice-cold phosphate-buffered saline, blotted dry, weighed, and frozen. Plasma and brain samples are stored at -80°C before bioanalytical analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

232.15

Formula

C₁₁H₁₅Cl₂N

CAS No.

846589-98-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 2.4 mg/mL

Lorcaserin hydrochloride is dissolved in sterile 0.9% saline[3].

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

References

Purity: 99.95%

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Product Name:
Lorcaserin Hydrochloride
Cat. No.:
HY-15368
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