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Details

Stereochemistry RACEMIC
Molecular Formula C21H24N2O2.ClH
Molecular Weight 372.888
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LY-272015 hydrochloride

SMILES

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

InChI

InChIKey=BKAZOTIBKRWLQA-UHFFFAOYSA-N
InChI=1S/C21H24N2O2.ClH/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;1H

HIDE SMILES / InChI

Molecular Formula C21H24N2O2
Molecular Weight 336.4275
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

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

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

PubMed

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
Record UNII
5NV3JP3GP6
Record Status Validated (UNII)
Record Version