LY-272015 FREE BASE

Details

Stereochemistry	RACEMIC
Molecular Formula	C21H24N2O2
Molecular Weight	336.4275
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=CC=C(CC2NCCC3=C2NC4=CC=C(C)C=C34)C=C1OC

InChI

InChIKey=GDAJGLDMCDMPIR-UHFFFAOYSA-N

InChI=1S/C21H24N2O2/c1-13-4-6-17-16(10-13)15-8-9-22-18(21(15)23-17)11-14-5-7-19(24-2)20(12-14)25-3/h4-7,10,12,18,22-23H,8-9,11H2,1-3H3

HIDE SMILES / InChI

Molecular Formula	C21H24N2O2
Molecular Weight	336.4275
Charge	0
Count

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

Description
Sources: Cohen ML, Schenck KW, Mabry TE, Nelson DL, Audia JE (1996) LY272015, a potent, selective and orally active 5-HT2B receptor antagonist. J Ser Res 3:131–144. | https://www.ncbi.nlm.nih.gov/pubmed/8709108
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/10070078 | https://www.ncbi.nlm.nih.gov/pubmed/12235249

LY-272015 is an antagonist at serotonin 5-HT2B receptor. LY-272015 exerts antihypertensive action in animal models.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Serotonin 2b (5-HT2b) receptor 60 Target ID: CHEMBL1833 Sources: Cohen ML, Schenck KW, Mabry TE, Nelson DL, Audia JE (1996) LY272015, a potent, selective and orally active 5-HT2B receptor antagonist. J Ser Res 3:131–144. \| https://www.ncbi.nlm.nih.gov/pubmed/8709108	Antagonist 2849

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 575 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10070078 https://www.ncbi.nlm.nih.gov/pubmed/12235249	Primary		Preclinical	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Signal Transduction Mechanism for Serotonin 5-HT2B Receptor-Mediated DNA Synthesis and Proliferation in Primary Cultures of Adult Rat Hepatocytes.	2016	26567725
5-HT is a potent relaxant in rat superior mesenteric veins.	2015-02	25692021
5HT(2A) and 5HT(2B) receptors contribute to serotonin-induced vascular dysfunction in diabetes.	2012	23346101
Expression and function of serotonin 2A and 2B receptors in the mammalian respiratory network.	2011	21789169
Endogenous 5-HT2B receptor activation regulates neonatal respiratory activity in vitro.	2006-08	16758492
Characterization of the contractile 5-hydroxytryptamine receptor in the renal artery of the normotensive rat.	2004-04	14724222
5-Hydroxytryptamine(2B) receptor function is enhanced in the N(omega)-nitro-L-arginine hypertensive rat.	2002-10	12235249
5-HT2B-receptor antagonist LY-272015 is antihypertensive in DOCA-salt-hypertensive rats.	1999-03	10070078

Patents

Sample Use Guides

In Vivo Use Guide

In chronically instrumented rats, the 5-HT2B-receptor antagonist LY-272015 (0.3, 1.0, and 3.0 mg/kg iv at 30-min intervals) was given cumulatively 1 time/wk during 4 wk of continued DOCA-salt treatment. LY-272015 did not reduce blood pressure of the sham-treated rats at any time or dose. However, LY-272015 (1.0 and 3. 0 mg/kg) significantly reduced mean blood pressure in a subgroup of week 3 (-20 mmHg) and week 4 DOCA-salt (-40 mmHg) rats that had extremely high blood pressure (mean arterial blood pressure approximately 200 mmHg).

Route of Administration: Intravenous

In Vitro Use Guide

LY272015 0.1 uM completely inhibited 5-HT or BW723C86 induced hepatocyte DNA synthesis and proliferation.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 16:18:32 GMT 2025` Edited by `admin` on `Wed Apr 02 16:18:32 GMT 2025`
Record UNII	6W6AEG3W3E
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

LY-272015 FREE BASE

Common Name

English

1-[(3,4-Dimethoxyphenyl)methyl]-2,3,4,9-tetrahydro-6-methyl-1H-pyrido[3,4-b]indole

Preferred Name

English

1H-Pyrido[3,4-b]indole, 1-[(3,4-dimethoxyphenyl)methyl]-2,3,4,9-tetrahydro-6-methyl-

Systematic Name

English

1H-Pyrido[3,4-b]indole, 1-[(3,4-dimethoxyphenyl)methyl]-2,3,4,9-tetrahydro-6-methyl-, (±)-

Systematic Name

English

Code System Code Type Description

FDA UNII

6W6AEG3W3E