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aliskiren hemifumarate

Known as: Aliskiren Fumarate, Bis((2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-8-methyl-2-(1-methylethyl)nonanamide) (2E)-but-2-enedioate 
An orally active nonpeptide renin inhibitor with antihypertensive activity. Aliskiren selectively binds to the S3 sub-pocket of renin, an enzyme in… Expand
National Institutes of Health

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Renin Inhibitors [MoA]

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Tekamlo

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aliskiren

Papers overview

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2014
2014
Prediction and modeling of effects on the QTc interval for clinical safety margin assessment, based on single-ascending-dose study data with AZD3839.
Corrected QT interval (QTc) prolongation in humans is usually predictable based on results from preclinical findings. This study… Expand
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2011
2011
Phenyl ring-substituted lobelane analogs: inhibition of [³H]dopamine uptake at the vesicular monoamine transporter-2.
Lobeline attenuates the behavioral effects of methamphetamine via inhibition of the vesicular monoamine transporter (VMAT2). To… Expand
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2009
2009
Inhibition of monoamine oxidases desensitizes 5-HT1A autoreceptors and allows nicotine to induce a neurochemical and behavioral sensitization.
Although nicotine is generally considered to be the main compound responsible for addictive properties of tobacco, experimental… Expand
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2006
2006
A novel, selective, and orally available antagonist for CC chemokine receptor 3.
CC chemokine ligand 11 (CCL11/eotaxin) and other CC chemokine receptor 3 (CCR3) ligands (CCL24/eotaxin-2, CCL26/eotaxin-3, CCL13… Expand
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2005
2005
Pharmacologic properties of YM218, a novel, potent, nonpeptide vasopressin V1A receptor-selective antagonist.
The pharmacologic profile of YM218, (Z)-4'-{4,4-difluoro-5-[2-oxo-2-(4-piperidinopiperidino)ethylidene]-2,3,4,5-tetrahydro-1H-1… Expand
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2003
2003
Contribution of 5-hydroxytryptamine1B receptors and 20-hydroxyeiscosatetraenoic acid to fall in cerebral blood flow after subarachnoid hemorrhage.
BACKGROUND AND PURPOSE This study examined the interaction between 5-hydroxytryptamine1B (5-HT1B) receptors and 20… Expand
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1997
1997
Repeated DOI and SR 46349B treatments do not affect elevated plus-maze anxiety despite opposite effects on cortical 5-HT2A receptors.
We report the consequences of a 4-day treatment (b.i.d) with the 5-HT2A,2B,2C receptor agonist 1-(2,5-dimethoxy-4-iodophenyl)-2… Expand
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1994
1994
Further evidence that various 5-HT receptor subtypes modulate central respiratory activity: in vitro studies with SR 46349B.
The ability of SR 46349B [trans,4-([3Z)3-(2-dimethylaminoethyl)oxyimino- 3(2-flurophenyl)propen-1-yl]phenol hemifumarate], a 5… Expand
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1993
1993
Up-regulation of 5-HT2 receptors in the rat brain by repeated administration of SR 46349B, a selective 5-HT2 receptor antagonist.
Chronic administration (twice a day for three days and on the morning of the fourth day) of SR 46349B (trans-4-[(3Z)3-(2… Expand
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1976
1976
Comparison of the action of BD 40 A and some other beta-adrenoceptor stimulants on the isolated trachea and atria of the guinea pig.
3-Formylamino-4-hydroxy-a-(N-1-methyl-2-p-methoxyphenethyl-aminomethyl)-benzylalcohol hemifumarate (BD 40A) was compared with… Expand
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