LIDANSERIN

Details

Stereochemistry	RACEMIC
Molecular Formula	C26H31FN2O4
Molecular Weight	454.5337
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=C(OCCCN2CCC(CC2)C(=O)C3=CC=C(F)C=C3)C=C(C=C1)C4CNC(=O)C4

InChI

InChIKey=JDYWZVJXSMADHP-UHFFFAOYSA-N

InChI=1S/C26H31FN2O4/c1-32-23-8-5-20(21-16-25(30)28-17-21)15-24(23)33-14-2-11-29-12-9-19(10-13-29)26(31)18-3-6-22(27)7-4-18/h3-8,15,19,21H,2,9-14,16-17H2,1H3,(H,28,30)

HIDE SMILES / InChI

Molecular Formula	C26H31FN2O4
Molecular Weight	454.5337
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: https://apps.who.int/iris/bitstream/handle/10665/275695/WHO-EMP-RHT-TSN-2018.1-eng.pdf | https://www.ncbi.nlm.nih.gov/pubmed/3240721 | https://www.ncbi.nlm.nih.gov/pubmed/2902861

Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist. In conscious spontaneously hypertensive rats intravenous injection of lidanserin caused dose-dependent blood pressure reductions. Lidanserin antagonises the excitatory effect of synaptically released 5-HT on central sympathoexcitatory neurons. Lidanserin is a potential antihypertensive compound which combines vasodilatatory effects due to selective alpha 1-receptor antagonistic action and platelet antiaggregatory, antivasospastic, and vasoprotective properties due to selective 5-HT2-receptor blockade.

Approval Year

PubMed

Title	Date	PubMed
Contribution of serotonergic systems to maintenance of blood pressure in anaesthetised normotensive Wistar Kyoto and conscious spontaneously hypertensive rats.	1988	3240721
Pharmacological profile of a new potent 5-hydroxytryptamine (5-HT2) alpha 1-receptor antagonist.	1988 Jun	2902861
Anxiolytics reverse the acceleration of ejaculation resulting from enforced intercopulatory intervals in rats.	1991 Apr	1675059

Sample Use Guides

In Vivo Use Guide

Single dose 0.3, 1.0 and 3.0 mg/kg

Route of Administration: Intravenous

Substance Class	Chemical Created by `admin` on `Fri Dec 15 16:15:14 GMT 2023` Edited by `admin` on `Fri Dec 15 16:15:14 GMT 2023`
Record UNII	80O1E9JZLN
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

LIDANSERIN

Official Name

English

2-PYRROLIDINONE, 4-(3-(3-(4-(4-FLUOROBENZOYL)-1-PIPERIDINYL)PROPOXY)-4-METHOXYPHENYL)-

Systematic Name

English

lidanserin [INN]

Common Name

English

ZK33839

Code

English

4-(3-(3-(4-(4-FLUOROBENZOYL)-1-PIPERIDINYL)PROPOXY)-4-METHOXYPHENYL)-2-PYRROLIDINONE

Common Name

English

ZK-33839

Code

English

(±)-4-(3-(3-(4-(P-FLUOROBENZOYL)PIPERIDINO)PROPOXY)-4-METHOXYPHENYL)-2-PYRROLIDINONE

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C66885