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=CC=CC=C2C(=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 87 Target ID: CHEMBL2095200 Sources: https://www.ncbi.nlm.nih.gov/pubmed/6494139 \| https://www.ncbi.nlm.nih.gov/pubmed/7493607	Antagonist 2778
Adrenergic receptor alpha-1 169 Target ID: CHEMBL2094251 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7493607	Antagonist 2778

PubMed

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

Substance Class	Chemical Created by `admin` on `Fri Dec 15 15:42:02 UTC 2023` Edited by `admin` on `Fri Dec 15 15:42:02 UTC 2023`
Record UNII	6SNR96E409
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PELANSERIN

Official Name

English

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

Systematic Name

English

pelanserin [INN]

Common 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