An OX2R antagonist; selective for OX2R over OX1R (IC50s = 18 and 1

MK-1064 – 1 mg

Brand:
Cayman
CAS:
1207253-08-4
Storage:
-20
UN-No:
Non-Hazardous - /

MK-1064 is an orexin 2 receptor (OX2R) antagonist that is selective for OX2R over OX1R (IC50s = 18 and 1,789 nM, respectively).{39919} It decreases the amount of time spent in active wake and increases the time spent in rapid eye movement (REM) sleep and slow-wave sleep (SMS) in mice, rats, dogs, and rhesus monkeys when administered at doses of 100, 20, 1, and 10 mg/kg, respectively. MK-1064 (30 mg/kg) inhibits restraint stress-induced increases in plasma adrenocorticotropic hormone (ACTH) levels and struggle behavior, as well as decreases in body weight, in rats expressing the hM3Dq designer receptor exclusively activated by designer drugs (DREADD) activated by clozapine N-oxide (CNO; Item No. 16882) in orexin neurons.{39920}  

 

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Description

An OX2R antagonist; selective for OX2R over OX1R (IC50s = 18 and 1,789 nM, respectively); decreases the amount of time spent in active wake and increases the time spent in REM sleep and SMS in mice, rats, dogs, and rhesus monkeys at 100, 20, 1, and 10 mg/kg, respectively; inhibits restraint stress-induced increases in plasma ACTH levels and struggle behavior, as well as decreases in body weight, at 30 mg/kg in rats expressing the hM3Dq DREADD activated by CNO in orexin neurons

Formal name: 5”-chloro-N-[(5,6-dimethoxy-2-pyridinyl)methyl]-[2,2′:5′,3”-terpyridine]-3′-carboxamide

Synonyms: 

Molecular weight: 461.9

CAS: 1207253-08-4

Purity: ≥98%

Formulation: A crystalline solid

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

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