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Details

Stereochemistry ACHIRAL
Molecular Formula C9H15N5.C4H4O4
Molecular Weight 309.3211
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of ALVAMELINE MALEATE

SMILES

OC(=O)\C=C/C(O)=O.CCN1N=NC(=N1)C2=CCCN(C)C2

InChI

InChIKey=YKFYFAAWVQGVTP-BTJKTKAUSA-N
InChI=1S/C9H15N5.C4H4O4/c1-3-14-11-9(10-12-14)8-5-4-6-13(2)7-8;5-3(6)1-2-4(7)8/h5H,3-4,6-7H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1-

HIDE SMILES / InChI

Description

Alvameline is a partial agonist of the M1 mAChR that also displays M2/M3 antagonist effects. It readily crosses the blood-brain barrier. It has an effect profile that makes it of interest to test its ability to counteract bladder overactivity in humans. Behaviorally, alvameline has been shown to significantly improve Morris water maze (MWM) performance in both young and ageimpaired rats. It failed to improve cognition in patients with mild to moderate Alzheimer's disease.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown
Primary
Unknown

T1/2

ValueDoseCo-administeredAnalytePopulation
3.1 h
125 mg 3 times / day multiple, oral
ALVAMELINE serum
Homo sapiens
3.7 h
150 mg 3 times / day multiple, oral
ALVAMELINE serum
Homo sapiens

Doses

AEs

Overview

OverviewOther

Other InhibitorOther SubstrateOther Inducer







Drug as victim

PubMed

Sample Use Guides

In Vivo Use Guide
25, 50, or 100 mg three times a day
Route of Administration: Oral
In Vitro Use Guide
Radioligand binding experiments demonstrated a small difference in affinity for Alvameline in the parotid gland compared with the bladder, the pKi values being 6.2 versus 6.5 (n=4).