WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H584266
CAS#: 117086-68-7
Description: Ricasetron, also known as Brl 46470, is antiemetic and axiolytic.
Hodoodo Cat#: H584266
Name: Ricasetron
CAS#: 117086-68-7
Chemical Formula: C19H27N3O
Exact Mass: 313.22
Molecular Weight: 313.445
Elemental Analysis: C, 72.81; H, 8.68; N, 13.41; O, 5.10
This product is not in stock, which may be available by custom synthesis.
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Synonym: Ricasetron; Brl 46470; Brl46470; Brl-46470
IUPAC/Chemical Name: 1H-Indole-1-carboxamide, 2,3-dihydro-3,3-dimethyl-N-(8-methyl-8-azabicyclo(3.2.1)oct-3-yl)-, endo-
InChi Key: ILXWRFDRNAKTDD-UHFFFAOYSA-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)
SMILES Code: O=C(N1CC(C)(C)C2=C1C=CC=C2)NC3CC(N4C)CCC4C3
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 313.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Bermudez J, Sanger GJ. Prolonged anti-emetic activity and 5-HT3-receptor antagonism by BRL 46470 in conscious ferrets. J Pharm Pharmacol. 1994 Jun;46(6):520-1. PubMed PMID: 7932054.
2: Kurata K, Ashby CR Jr, Oberlender R, Tanii Y, Kurachi M, Rini NJ, Strecker RE. The characterization of the effect of locally applied N-methylquipazine, a 5-HT3 receptor agonist, on extracellular dopamine levels in the anterior medial prefrontal cortex in the rat: an in vivo microdialysis study. Synapse. 1996 Dec;24(4):313-21. PubMed PMID: 10638822.
3: Blackburn TP, Baxter GS, Kennett GA, King FD, Piper DC, Sanger GJ, Thomas DR, Upton N, Wood MD. BRL 46470A: a highly potent, selective and long acting 5-HT3 receptor antagonist with anxiolytic-like properties. Psychopharmacology (Berl). 1993;110(3):257-64. PubMed PMID: 7831418.
4: Setem J, Pinheiro AP, Motta VA, Morato S, Cruz AP. Ethopharmacological analysis of 5-HT ligands on the rat elevated plus-maze. Pharmacol Biochem Behav. 1999 Mar;62(3):515-21. PubMed PMID: 10080245.
5: Gargiulo PA, Viana MB, Graeff FG, Silva MA, Tomaz C. Effects of anxiety and memory of systemic and intra-amygdala injection of 5-HT3 receptor antagonist BRL 46470A. Neuropsychobiology. 1996;33(4):189-95. PubMed PMID: 8840342.
6: Link CG, Leigh TJ, Dennison JK. The effects of BRL 46470A, a novel 5-HT3 receptor antagonist, and lorazepam on psychometric performance and the EEG. Br J Clin Pharmacol. 1993 Apr;35(4):395-9. PubMed PMID: 8485019; PubMed Central PMCID: PMC1381550.
7: de Souza Silva M, Guimarães FS, Graeff FG, Tomaz C. Absence of amnestic effect of an anxiolytic 5-HT3 antagonist (BRL 46470A) injected into basolateral amygdala, as opposed to diazepam. Behav Brain Res. 1993 Dec 31;59(1-2):141-5. PubMed PMID: 8155281.
8: Newberry NR, Watkins CJ, Sprosen TS, Blackburn TP, Grahame-Smith DG, Leslie RA. BRL 46470 potently antagonizes neural responses activated by 5-HT3 receptors. Neuropharmacology. 1993 Aug;32(8):729-35. PubMed PMID: 8413836.
9: Gao B, Cutler MG. 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. PubMed PMID: 1630589.
10: Gao B, Cutler MG. Effects of chlordiazepoxide, buspirone and the 5-HT3 receptor antagonist, BRL 46470, on the behaviour of oestrous and dioestrous female mice when encountering male partners. Neuropharmacology. 1993 Oct;32(10):969-75. PubMed PMID: 7905193.
11: Blackshaw LA, Nisyrios V, Dent J. Responses of ferret lower esophageal sphincter to 5-hydroxytryptamine: pathways and receptor subtypes. Am J Physiol. 1995 Jun;268(6 Pt 1):G1004-11. PubMed PMID: 7611399.
12: Nucci-da-Silva LP, Guimarães FS, Del Bel EA. Serotonin modulation of catalepsy induced by N(G)-nitro-L-arginine in mice. Eur J Pharmacol. 1999 Aug 20;379(1):47-52. PubMed PMID: 10499370.
13: Sanger GJ, Wardle KA. Constipation evoked by 5-HT3-receptor antagonism: evidence for heterogeneous efficacy among different antagonists in guinea-pigs. J Pharm Pharmacol. 1994 Aug;46(8):666-70. PubMed PMID: 7815281.
14: Watkins CJ, Newberry NR. Multiple 5-HT receptors in the guinea-pig superior cervical ganglion. Br J Pharmacol. 1996 Jan;117(1):21-8. PubMed PMID: 8825338; PubMed Central PMCID: PMC1909384.
15: Gao B, Cutler MG. Effects of acute administration of the 5-HT3 receptor antagonist, BRL 46470A, on the behaviour of mice in a two compartment light-dark box and during social interactions in their home cage and an unfamiliar neutral cage. Neuropharmacology. 1992 Aug;31(8):743-8. PubMed PMID: 1356251.
16: Yuan SY, Bornstein JC, Furness JB. Investigation of the role of 5-HT3 and 5-HT4 receptors in ascending and descending reflexes to the circular muscle of guinea-pig small intestine. Br J Pharmacol. 1994 Aug;112(4):1095-100. PubMed PMID: 7952869; PubMed Central PMCID: PMC1910247.
17: Silverstone PH, Cowen PJ. The 5-HT3 antagonist, BRL 46470 does not attenuate m-chlorophenylpiperazine (mCPP)-induced changes in human volunteers. Biol Psychiatry. 1994 Sep 1;36(5):309-16. PubMed PMID: 7993957.
18: Steward LJ, Ge J, Bentley KR, Barber PC, Hope AG, Lambert JJ, Peters JA, Blackburn TP, Barnes NM. 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. PubMed PMID: 8528560; PubMed Central PMCID: PMC1909107.
19: Gifford AN, Wang RY. The effect of 5-HT3 receptor antagonists on the morphine-induced excitation of A10 dopamine cells: electrophysiological studies. Brain Res. 1994 Feb 28;638(1-2):325-8. PubMed PMID: 8199870.
20: Banner SE, Sanger GJ. Differences between 5-HT3 receptor antagonists in modulation of visceral hypersensitivity. Br J Pharmacol. 1995 Jan;114(2):558-62. PubMed PMID: 7881756; PubMed Central PMCID: PMC1510257.
