Related CAS #
42877-18-9 (HCl); 2208-51-7 (free base)
Synonym
Pelanserin Free Base; Pelanserine; Pelanserinum
IUPAC/Chemical Name
2,4(1H,3H)-Quinazolinedione, 3-(3-(4-phenyl-1-piperazinyl)propyl)-
InChi Key
WPKPLSFHHBBLRY-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H24N4O2/c26-20-18-9-4-5-10-19(18)22-21(27)25(20)12-6-11-23-13-15-24(16-14-23)17-7-2-1-3-8-17/h1-5,7-10H,6,11-16H2,(H,22,27)
SMILES Code
O=C(N1CCCN2CCN(C3=CC=CC=C3)CC2)NC4=C(C=CC=C4)C1=O
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
364.45
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 |
1: Aguirre Hernández G, Somanathan R, Bernès S. Pelanserin: 3-[3-(4-phenyl- piperazin-1-yl)prop-yl]quinazoline-2,4(1H,3H)-dione. Acta Crystallogr Sect E Struct Rep Online. 2014 Jul 23;70(Pt 8):o878. doi: 10.1107/S160053681401602X. PMID: 25249922; PMCID: PMC4158516.
2: Espinoza R, Hong E, Villafuerte L. Influence of admixed citric acid on the release profile of pelanserin hydrochloride from HPMC matrix tablets. Int J Pharm. 2000 May 25;201(2):165-73. doi: 10.1016/s0378-5173(00)00406-3. PMID: 10878323.
3: Flores Murrieta FJ, Castañeda Hernández G, Hong E. Farmacocinetica y efecto antihipertensivo de la pelanserina en perros [Pharmacokinetics and antihypertensive effect of pelanserin in dogs ]. Arch Inst Cardiol Mex. 1990 Jul-Aug;60(4):347-51. Spanish. PMID: 2268171.
4: Villalobos-Molina R, Ibarra M, Hong E. The 5-HT2 receptor antagonist, pelanserin, inhibits alpha 1-adrenoceptor-mediated vasoconstriction in vitro. Eur J Pharmacol. 1995 Apr 24;277(2-3):181-5. doi: 10.1016/0014-2999(95)00074-u. PMID: 7493607.
5: Flores-Murrieta FJ, Castañeda-Hernández G, Hong E. Pharmacokinetics and antihypertensive effect of oral pelanserin in renal hypertensive dogs. Arzneimittelforschung. 1992 Sep;42(9):1105-8. PMID: 1445477.
6: Flores-Murrieta FJ, Herrera JE, Castañeda-Hernández G, Hong E. Pharmacokinetics of pelanserin in healthy volunteers. Proc West Pharmacol Soc. 1992;35:113-6. PMID: 1502209.
7: Hong E, Castillo C, Flores E, Mercedes F. Receptores serotoninérgicos y enfermedades cardiovasculares [Serotoninergic receptors and cardiovascular diseases]. Gac Med Mex. 1994 May-Jun;130(3):131-3. Spanish. PMID: 7657075.
8: Flores-Murrieta FJ, Hong E, Castañeda-Hernández G. Sensitive high-performance liquid chromatographic assay of pelanserin, a novel antihypertensive agent, in plasma samples. J Chromatogr. 1988 Jun 24;428(1):167-72. doi: 10.1016/s0378-4347(00)83903-1. PMID: 3170670.
9: Flores-Murrieta FJ, Castañeda-Hernández G, Hong E. Determination of pelanserin in human plasma by high-performance liquid chromatography with amperometric detection. J Chromatogr. 1990 Jun 29;528(2):501-8. doi: 10.1016/s0378-4347(00)82410-x. PMID: 2384588.
10: Campos-Lara G, Caracheo F, Valencia-Sánchez A, Ponce-Monter H. The sensitivity of rat uterus to serotonin in vitro is a late estrogenic response. Arch Invest Med (Mex). 1990 Jan-Mar;21(1):71-5. PMID: 2222119.