pelanserin
Description
Pelanserin is a selective 5-HT2A receptor antagonist that has shown promise in the treatment of Alzheimer's disease and other neurodegenerative disorders. It has been shown to improve cognitive function and reduce amyloid-beta plaque formation in animal models of Alzheimer's disease. The mechanism of action of pelanserin is believed to be related to its ability to block the activation of the 5-HT2A receptor, which is known to be involved in the pathogenesis of Alzheimer's disease. Pelanserin is currently in clinical trials for the treatment of Alzheimer's disease.'
pelanserin: RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 65435 |
| CHEMBL ID | 2110706 |
| SCHEMBL ID | 120877 |
| MeSH ID | M0127148 |
Synonyms (32)
| Synonym |
|---|
| pelanserin |
| 3-[3-(4-phenylpiperazin-1-yl)propyl]-1h-quinazoline-2,4-dione |
| pelanserinum [latin] |
| pelanserine |
| 6snr96e409 , |
| 2208-51-7 |
| 2,4(1h,3h)-quinazolinedione, 3-(3-(4-phenyl-1-piperazinyl)propyl)- |
| pelanserinum |
| pelanserine [french] |
| pelanserina [spanish] |
| unii-6snr96e409 |
| pelanserin [inn] |
| pelanserina |
| 3-(3-(4-phenyl-1-piperazinyl)propyl)-2,4(1h,3h)-quinazolinedione |
| smr004703317 |
| MLS006011551 |
| SCHEMBL120877 |
| WPKPLSFHHBBLRY-UHFFFAOYSA-N |
| CHEMBL2110706 |
| Z379486794 |
| DTXSID60176578 |
| AKOS027327171 |
| SR-01000945189-2 |
| sr-01000945189 |
| SR-01000945189-1 |
| 2,4(1h,3h)-quinazolinedione, 3-[3-(4-phenyl-1-piperazinyl)propyl]- |
| 3-[3-(4-phenylpiperazin-1-yl)propyl]-1h-quinazoline-2,4-dionehydrochloride |
| 3-[3-(4-phenylpiperazin-1-yl)propyl]quinazoline-2,4(1h,3h)-dione |
| 3-(3-(4-phenylpiperazin-1-yl)propyl)quinazoline-2,4(1h,3h)-dione |
| Q15634029 |
| 3-[3-(4-phenylpiperazin-1-yl)propyl]-1,2,3,4-tetrahydroquinazoline-2,4-dione |
| EN300-2007609 |
Research Excerpts
Overview
Pelanserin is a weakly basic experimental drug with a short half-life. It was developed using hydroxypropyl methylcellulose (HPMC) and citric acid.
| Excerpt | Reference | Relevance |
|---|---|---|
| "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. " | ( Influence of admixed citric acid on the release profile of pelanserin hydrochloride from HPMC matrix tablets. Espinoza, R; Hong, E; Villafuerte, L, 2000) | 1.99 |
Pharmacokinetics
The pharmacokinetic and pharmacodynamic profiles of pelanserin allow to predict that this drug could have a place in the therapeutics of arterial hypertension. After the first dose, pelanserserin was absorbed reaching a Cmax value of 39.
| Excerpt | Reference | Relevance |
|---|---|---|
| " After the first dose, pelanserin was absorbed reaching a Cmax value of 39." | ( Pharmacokinetics and antihypertensive effect of oral pelanserin in renal hypertensive dogs. Castañeda-Hernández, G; Flores-Murrieta, FJ; Hong, E, 1992) | 0.84 |
| " The pharmacokinetic and pharmacodynamic profiles of pelanserin allow to predict that this drug could have a place in the therapeutics of arterial hypertension." | ( [Pharmacokinetics and antihypertensive effect of pelanserin in dogs ]. Castañeda Hernández, G; Flores Murrieta, FJ; Hong, E, ) | 0.64 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " Pelanserin bioavailability after oral dosing was about 30%, this could be due to a poor absorption from the gastrointestinal tract or to an important hepatic biotransformation by first pass effect." | ( [Pharmacokinetics and antihypertensive effect of pelanserin in dogs ]. Castañeda Hernández, G; Flores Murrieta, FJ; Hong, E, ) | 1.3 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " Pelanserin bioavailability after oral dosing was about 30%, this could be due to a poor absorption from the gastrointestinal tract or to an important hepatic biotransformation by first pass effect." | ( [Pharmacokinetics and antihypertensive effect of pelanserin in dogs ]. Castañeda Hernández, G; Flores Murrieta, FJ; Hong, E, ) | 1.3 |
Research
Studies (12)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 5 (41.67) | 18.7374 |
| 1990's | 5 (41.67) | 18.2507 |
| 2000's | 2 (16.67) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 11.51
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (11.51) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 14 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||