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Enzyme
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Target Concepts:
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Query: UMLS:C0917801 (
insomnia
)
10,606
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
Insomnia
is one of the most common sleep problems with an estimated prevalence of 10%-15% in the general population. Although adenosine A
2A
receptor (A
2A
R) agonists strongly induce sleep, their cardiovascular effects preclude their use in treating sleep disorders. Enhancing endogenous A
2A
R signaling, however, may be an alternative strategy for treating
insomnia
, because adenosine levels in the brain accumulate during wakefulness. In the present study, we found that 3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)benzoic acid, denoted A
2A
R positive allosteric modulator (PAM)-1, enhanced adenosine signaling at the A
2A
R and induced slow wave sleep (SWS) without affecting body temperature in wild-type male mice after intraperitoneal administration, whereas the SWS-inducing effect of this benzoic acid derivative was abolished in A
2A
R KO mice. In contrast to the A
2A
R agonist CGS 21680, the A
2A
R
PAM-1
did not affect blood pressure or heart rate. These findings indicate that enhancing A
2A
R signaling promotes SWS without cardiovascular effects. Therefore, small molecules that allosterically modulate A
2A
Rs could help people with
insomnia
to fall asleep.
...
PMID:Enhancing endogenous adenosine A
2A
receptor signaling induces slow-wave sleep without affecting body temperature and cardiovascular function. 3110 60
