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Table 12.1 In vivo cardiovascular effects of barrs, underlying molecular mechanisms, and therapeutic implications for cardiovascular diseases
Tissue and
receptor
b arr
isoform
Action on
receptor
Signaling
pathway(s) affected
Desirable
intervention (disease)
In vivo effect
Refs.
VSM
a 2B AR
b arr1/2
Desensitizer N/A
Vasodilation;
#
vasoconstriction
Stimulation (HTN)
10,11
Adrenal
a 2 AR
b arr1
Desensitizer N/A
"
Catecholamine secretion
Inhibition (HF)
15-18
Central
SNS a 2 AR
b arr2
Signal
transducer
Unknown,
spinophilin?
Sedation of antihypertensive
centrally acting a 2 AR agonists
Inhibition (HTN)
19,20
Cardiac
b 1 - and
b 2 ARs
b arr1/2
(mainly
b arr1)
Desensitizer N/A
#
Cardiac contractility
Inhibition (HF)
21-24
Cardiac
b 1 AR
b arr2
Signal
transducer
EGFR transactivation,
ERK
"
Cardiomyocyte survival-
proliferation
Stimulation (HF)
25-27
Cardiac
b 2 AR
b arr1/2
Desensitizer N/A
#
Cardiomyocyte survival-
proliferation
Inhibition (HF?)
21,24,27
Cardiac
b 2 AR
b arr1/2
Signal
transducer
ERK, NF- k B
inhibition
"
Cardiomyocyte survival-
proliferation
Stimulation (HF?)
28-30
Cardiac
AT 1 R
b arr2
Signal
transducer
EGFR transactivation,
ERK, Akt
"
Cardiac contractility-
function-survival-proliferation
Stimulation or
inhibition of b arr1
(HF)
31-34
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