A histamine H3 receptor antagonist (Kis = 1.17 and 7.08 nM for human and rat receptors

JNJ-10181457 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
544707-20-2
Storage:
-20
UN-No:
Non-Hazardous - /

JNJ-10181457 is an antagonist of histamine H3 receptors (Kis = 1.17 and 7.08 nM for human and rat receptors, respectively).{49250} It increases extracellular norepinephrine and acetylcholine levels in the frontal cortex of rats when administered subcutaneously at a dose of 10 mg/kg. JNJ-10181457 (1.25-10 mg/kg, p.o.) reduces the number of cataplectic attacks and time spent in cataplexy in familial narcoleptic Dobermans. In mice, JNJ-10181457 (10 mg/kg) decreases the time spent in the open areas of the elevated zero maze, as well as increases locomotor activity in an open field test.{49251} It also inhibits LPS-induced increases in time spent immobile in the tail suspension test in mice.{49252}  

 

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SKU: 11997 - 5 mg Category:

Description

A histamine H3 receptor antagonist (Kis = 1.17 and 7.08 nM for human and rat receptors, respectively); increases extracellular norepinephrine and acetylcholine levels in the frontal cortex of rats at 10 mg/kg; reduces the number of cataplectic attacks and time spent in cataplexy in familial narcoleptic Dobermans at 1.25-10 mg/kg; decreases the time spent in the open areas of the elevated zero maze in mice at 10 mg/kg, as well as increases locomotor activity in an open field test; inhibits LPS-induced increases in time spent immobile in the tail suspension test in mice.

Formal name: 4-[[3-[4-(1-piperidinyl)-1-butyn-1-yl]phenyl]methyl]-morpholine, dihydrochloride

Synonyms:  RWJ 662733

Molecular weight: 385.4

CAS: 544707-20-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Behavioral Neuroscience|Depression||Research Area|Neuroscience|Behavioral Neuroscience|Sleep & Biological Rhythms

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