| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| Other Sizes |
| Targets |
5-HT3 receptors (Ki = 1.2 nM for displacement of [3H]-BRL46470 in rat cerebral cortex; Ki = 32 nM for displacement of [3H]-granisetron in rat entorhinal cortex) [1]
|
|---|---|
| ln Vitro |
- Ricasetron (BRL-46470) labeled a higher density of binding sites in rat brain homogenates compared to [3H]-granisetron, a typical 5-HT3 receptor ligand. Scatchard analysis of [3H]-BRL46470 binding in rat cerebral cortex showed a Bmax of 116 fmol/mg protein and a Kd of 0.5 nM, indicating high-affinity binding to 5-HT3 receptors [1]
- In competitive binding assays, unlabeled BRL-46470 displaced [3H]-granisetron from rat entorhinal cortex sites with a Ki of 32 nM, but was more potent in displacing [3H]-BRL46470 (Ki = 1.2 nM), suggesting selectivity for a subset of 5-HT3 receptors [1] |
| ln Vivo |
- Sub-chronic treatment with Ricasetron (BRL-46470) (1 mg/kg, intraperitoneal injection, once daily for 7 days) increased social interaction time in mice, as measured by paired encounters in a neutral arena. The effect was comparable to chlordiazepoxide but distinct from buspirone, suggesting modulation of anxiety-related social behavior [2]
- The drug did not alter locomotor activity at the tested dose, indicating that the increased social interaction was not due to nonspecific stimulation of movement [2] |
| Enzyme Assay |
- 5-HT3 receptor binding assay: Rat cerebral cortex or entorhinal cortex homogenates were prepared and incubated with [3H]-BRL46470 (0.1-5 nM) in buffer at 25°C for 60 minutes. Nonspecific binding was defined using excess unlabeled BRL-46470 (1 μM). Bound ligand was separated from free ligand by rapid filtration through glass fiber filters, and radioactivity was measured by liquid scintillation counting. For competition studies, unlabeled ligands (including BRL-46470) were added at concentrations ranging from 10-10 to 10-4 M, and Ki values were calculated using the Cheng-Prusoff equation [1]
|
| Animal Protocol |
Social behavior assay: Male mice were housed individually for 7 days before treatment. Ricasetron (BRL-46470) was dissolved in saline and administered intraperitoneally at 1 mg/kg once daily for 7 days. Control groups received saline. On day 7, pairs of mice (from the same treatment group) were placed in a novel arena, and social interaction (including sniffing, grooming, and following) was video-recorded for 10 minutes. Total interaction time was quantified by blinded observers [2]
|
| References |
[1]. Evidence that the atypical 5-HT3 receptor ligand, [3H]-BRL46470, labels additional 5-HT3 binding sites compared to [3H]-granisetron. Br J Pharmacol. 1995 Sep;116(2):1781-8.
[2]. Effects of sub-chronic treatment with chlordiazepoxide, buspirone and the 5-HT3 receptor antagonist, BRL 46470, on the social behaviour of mice. Neuropharmacology. 1992 Mar;31(3):207-13. |
| Additional Infomation |
- Ricasetron (BRL-46470) is classified as an atypical 5-HT3 receptor ligand because it can label a wider range of 5-HT3 binding sites compared to typical ligands such as granisetron [1]
- Its effects on social behavior suggest that it may have anxiolytic properties, but its exact mechanisms (other than 5-HT3 receptor regulation) remain unclear [2] |
| Molecular Formula |
C19H27N3O
|
|---|---|
| Molecular Weight |
313.445
|
| Exact Mass |
313.215
|
| Elemental Analysis |
C, 72.81; H, 8.68; N, 13.41; O, 5.10
|
| CAS # |
117086-68-7
|
| Related CAS # |
140865-88-9 (HCl)
|
| PubChem CID |
71785
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
478.4±45.0 °C at 760 mmHg
|
| Flash Point |
243.1±28.7 °C
|
| Vapour Pressure |
0.0±1.2 mmHg at 25°C
|
| Index of Refraction |
1.611
|
| LogP |
3.31
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
23
|
| Complexity |
463
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
O=C(N1CC(C)(C)C2=CC=CC=C12)NC1CC2CCC(N2C)C1
|
| InChi Key |
ILXWRFDRNAKTDD-GOOCMWNKSA-N
|
| InChi Code |
InChI=1S/C19H27N3O/c1-19(2)12-22(17-7-5-4-6-16(17)19)18(23)20-13-10-14-8-9-15(11-13)21(14)3/h4-7,13-15H,8-12H2,1-3H3,(H,20,23)/t13?,14-,15+
|
| Chemical Name |
3,3-dimethyl-N-[(1S,5R)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]-2H-indole-1-carboxamide
|
| Synonyms |
Brl-46470; BRL-46,470; Brl 46,470; Ricasetron; 117086-68-7; 3,3-dimethyl-N-[(1S,5R)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]-2H-indole-1-carboxamide; R92JB88O88; 3,3-Dimethyl-N-((1R,3r,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl)indoline-1-carboxamide; 3,3-Dimethyl-N-(8-methyl-8-azabicyclo[3.2.1]octan-3-yl)-2H-indole-1-carboxamide; Brl 46470; Ricasetron
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1903 mL | 15.9515 mL | 31.9030 mL | |
| 5 mM | 0.6381 mL | 3.1903 mL | 6.3806 mL | |
| 10 mM | 0.3190 mL | 1.5952 mL | 3.1903 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
