DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

Table 8–6
Characteristics for Adrenergic Receptor Subtypes
GENE LOCATION
IN HUMAN G-PROTEIN PRINCIPLE TISSUE SUBTYPE
SUBTYPE a CHROMOSOME COUPLING EFFECTORS LOCALIZATION DOMINANT EFFECTS b
α 1A
8p21-p11.2 Gα q
↑ PLC, ↑ PLA 2
Heart • Predominant receptor
(α 11
/α 14
/α 16
) ↑ Ca 2+ channels Liver causing contraction of
↑ Na + /H + exchanger Smooth muscle vascular smooth muscle
Modulation of K + Blood vessels • Promotes cardiac
channels Lung growth and structure
↑ MAPK Signaling Vas deferens • Vasoconstriction of large
Prostate
resistant arterioles in
Cerebellum skeletal muscle
Cortex
Hippocampus
α 1B
5q23-q32 Gα q
↑ PLC, ↑ PLA 2
Kidney • Most abundant subtype in
(α 11
/α 14
/α 16
) ↑ Ca 2+ channels Spleen heart
↑ Na + /H + exchanger Lung • Promotes cardiac growth
Modulation of K + Blood vessels and structure
channels
Cortex
↑ MAPK Signaling Brainstem
α 1D
20p13 Gα q
↑ PLC, ↑ PLA 2
Platelets • Predominant receptor
(α 11
/α 14
/α 16
) ↑ Ca 2+ channels Prostate causing vasoconstriction
↑ Na + /H + exchanger Aorta in aorta and coronary artery
Modulation of K + Coronary artery
channels
Cortex
↑ MAPK Signaling Hippocampus
α 2A
10q24-q26 Gα i
Family Inhibition of AC Platelets • Predominant inhibitory
Gα o
Family ↓ cAMP Sympathetic neurons receptor on sympathetic
(α o1
/α o2
) ↓ PKA activity Autonomic ganglia neurons
Pancreas
• Vasoconstriction of small
Coronary/CNS procapillary vessels in
vessels
skeletal muscle
Locus ceruleus
Brainstem
Spinal cord
α 2B
2q12-q13 Gα i
Family Inhibition of AC Liver • Predominant receptor
Gα o
Family ↓ cAMP Kidney mediating α 2
(α o1
/α o2
) ↓ PKA activity Blood vessels vasoconstriction
Coronary/CNS
vessels
Diencephalon
Pancreas
Platelets
α 2c
4p16 Gα i
Family Inhibition of AC Basal ganglia • Predominant receptor
(α 11
/α 12
/α 13
) ↓ cAMP Cortex modulating dopamine
Gα o
Family ↓ PKA activity Cerebellum neurotransmission
(α o1
/α o2
) Hippocampus • Predominant receptor
inhibiting hormone release
from adrenal medulla
(Continued)