PELANSERIN

Details

Stereochemistry	ACHIRAL
Molecular Formula	C21H24N4O2
Molecular Weight	364.4409
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O=C1NC2=C(C=CC=C2)C(=O)N1CCCN3CCN(CC3)C4=CC=CC=C4

InChI

InChIKey=WPKPLSFHHBBLRY-UHFFFAOYSA-N

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)

HIDE SMILES / InChI

Molecular Formula	C21H24N4O2
Molecular Weight	364.4409
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7493607 | https://www.ncbi.nlm.nih.gov/pubmed/1445477 | https://adisinsight.springer.com/drugs/800001361

Pelanserin is an antagonist of the serotonin 5-HT2 receptor and blocks alpha 1-adrenoceptor. Experiments on dogs have revealed that pelanserin showed adequate pharmacokinetic and pharmacodynamics profiles as an antihypertensive agent that is why the drug possessed potential therapeutic usefulness in the treatment of hypertension. Pelanserin was undergoing phase II clinical trials by Cinvestav in Mexico; however, these studied were discontinued.

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Serotonin 2 (5-HT2) receptor 90 Target ID: CHEMBL2095200 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6494139 \| https://www.ncbi.nlm.nih.gov/pubmed/7493607	Antagonist 2849
Adrenergic receptor alpha-1 171 Target ID: CHEMBL2094251 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7493607	Antagonist 2849

PubMed

Title	Date	PubMed
Carbopol 934-Sodium Alginate-Gelatin Mucoadhesive Ondansetron Tablets for Buccal Delivery: Effect of pH Modifiers.	2010-07	21218058
Influence of Organic Acids on Diltiazem HCl Release Kinetics from Hydroxypropyl Methyl Cellulose Matrix Tablets.	2010-07	21042476
Alkylation of 2,4-(1H,3H)-quinazolinediones with dialkyl carbonates under microwave irradiations.	2009-05-20	19471206
Mechanism of the antihypertensive effect of TR2515, a potent serotonin antagonist.	1984	6494139

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:05:58 GMT 2025` Edited by `admin` on `Mon Mar 31 18:05:58 GMT 2025`
Record UNII	6SNR96E409
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

pelanserin [INN]

Preferred Name

English

PELANSERIN

Official Name

English

3-(3-(4-PHENYL-1-PIPERAZINYL)PROPYL)-2,4(1H,3H)-QUINAZOLINEDIONE

Systematic Name

English

2,4(1H,3H)-QUINAZOLINEDIONE, 3-(3-(4-PHENYL-1-PIPERAZINYL)PROPYL)-

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C66885