Community hub
0 subscribers8 pages, 0 posts
Recent from talks
Be the first to start a discussion here.
Be the first to start a discussion here.
Be the first to start a discussion here.
Be the first to start a discussion here.
Contribute something
Welcome to the community hub built to collect knowledge and have discussions related to Pelanserin.
Nothing was collected or created yet.
Pelanserin
View on Wikipediafrom Wikipedia
 | |
| Clinical data | |
|---|---|
| Other names | TR2515; TR-2515 |
| Routes of administration | Oral[1] |
| Drug class | Serotonin 5-HT2A receptor antagonist; α1-Adrenergic receptor antagonist |
| ATC code |
|
| Pharmacokinetic data | |
| Onset of action | <1 hour (Tmax)[1] |
| Elimination half-life | 3.8 hours[1] |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C21H24N4O2 |
| Molar mass | 364.449 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
Pelanserin (developmental code name TR-2515) is a serotonin 5-HT2 and α1-adrenergic receptor antagonist which was under development for the treatment of hypertension but was never marketed.[2][3] Its development was discontinued in 2001.[2]
Pharmacology
[edit]Pharmacokinetics
[edit]The pharmacokinetics of pelanserin have been studied.[4] It has a relatively short elimination half-life.[5][4] The drug's time to peak levels was less than 1 hour and its half-life was 3.8 hours in a single subject in an analytical study.[1]
Chemistry
[edit]Synthesis
[edit]
Pelanserin (3) can be synthesized by a reaction between isatoic anhydride (1) and 1-(3-aminopropyl)-4-phenylpiperazine (2) in the presence of phosgene.[6][7][8][9][10][11][12][13]
See also
[edit]References
[edit]- ^ a b c d Flores-Murrieta FJ, Hong E, Castañeda-Hernández G (June 1988). "Sensitive high-performance liquid chromatographic assay of pelanserin, a novel antihypertensive agent, in plasma samples". Journal of Chromatography. 428 (1): 167–172. doi:10.1016/s0378-4347(00)83903-1. PMID 3170670.
- ^ a b "Pelanserin". AdisInsight. 30 August 2002. Retrieved 17 January 2026.
- ^ Villalobos-Molina R, Ibarra M, Hong E (April 1995). "The 5-HT2 receptor antagonist, pelanserin, inhibits alpha 1-adrenoceptor-mediated vasoconstriction in vitro". European Journal of Pharmacology. 277 (2–3): 181–185. doi:10.1016/0014-2999(95)00074-u. PMID 7493607.
- ^ a b Flores-Murrieta FJ, Herrera JE, Castañeda-Hernández G, Hong E (1992). "Pharmacokinetics of pelanserin in healthy volunteers". Proceedings of the Western Pharmacology Society. 35: 113–116. PMID 1502209.
- ^ Espinoza R, Hong E, Villafuerte L (May 2000). "Influence of admixed citric acid on the release profile of pelanserin hydrochloride from HPMC matrix tablets". International Journal of Pharmaceutics. 201 (2): 165–173. doi:10.1016/s0378-5173(00)00406-3. PMID 10878323.
Pelanserin is a weakly basic experimental drug with a short half-life and a prolonged release formulation was developed using hydroxypropyl methylcellulose (HPMC) and citric acid to set up a system bringing about gradual release of this drug.
- ^ Hayao S, Havera HJ, Strycker WG, Leipzig TJ, Kulp RA, Hartzler HE (November 1965). "New sedative and hypotensive 3-substituted 2,4(1H,3H)-quinazolinediones". Journal of Medicinal Chemistry. 8 (6): 807–815. doi:10.1021/jm00330a017. PMID 5885076.
- ^ Havera HJ, Vidrio H (December 1979). "Derivatives of 1,3-disubstituted 2,4(1H,3H)-quinazolinediones as possible peripheral vasodilators or antihypertensive agents". Journal of Medicinal Chemistry. 22 (12): 1548–1550. doi:10.1021/jm00198a024. PMID 231656.
- ^ Garcia JD, Somanathan R, Rivero IA, Aguirre G, Hellberg LH (2000). "Synthesis of Deuterium-Labeled Antihypertensive 3-(4-Phenyl-1′-Piperazinyl)-Propyl-2,4-Quinazolinedione". Synthetic Communications. 30 (15): 2707–2711. doi:10.1080/00397910008086895.
- ^ Li X, Lee YR, Kim SH (2011). "Concise Synthesis of Pelanserine, Goshuyuamide II, and Wuchuyuamide II with Quinazolinedione Nuclei". Bulletin of the Korean Chemical Society. 32 (9): 3480–3482. doi:10.5012/bkcs.2011.32.9.3480.
- ^ Cortez R, Rivero IA, Somanathan R, Aguirre G, Ramirez F, Hong E (1991). "Synthesis of Quinazolinedione Using Triphosgene". Synthetic Communications. 21 (2): 285–292. doi:10.1080/00397919108020823.
- ^ AT 269143B, "Verfahren zur Herstellung von neuen Chinazolindionderivaten und ihrer Säureadditionssalze bzw. ihrer entsprechenden Piperaziniumverbindungen [Process for the preparation of new quinazolinedione derivatives and their acid addition salts or their corresponding piperazinium compounds]", published 1969-03-10, assigned to Miles Laboratories, Inc.
- ^ US 3274194, Shin H, "Quinazolinedione derivatives", issued 20 September 1966, assigned to Bayer Corp.
- ^ US 3919425, Vidrio H, "Method of producing vasodilation using certain 3-substituted-quinazoline derivatives", issued 11 November 1975, assigned to Bayer Corp.