Receptors Flashcards
M1
Gq-coupled: neurons
• Decrease in membrane PIP2 inhibits potassium conductance (M-channel) in neurons
M2
Gi-coupled: heart and presynaptic nerve terminals
• Neurons: phosphorylation of Cav reduces transmitter release
• Heart: βɣ activates GIRK decreasing HR
M3
Gq-coupled: exocrine/sweat glands, oxyntic cells, smooth muscle
• Muscle contraction
• Glandular secretion
α1
Gq-coupled (NA≥Adr) • Vasoconstriction • Contraction of uterine smooth muscle • Relaxation of GI smooth muscle • Salivary secretion • Glycogenolysis
α2
Gi-coupled (Adr≥NA)
• Inhibits transmitter release (presynaptic)
β1
Gs-coupled (Adr=NA)
• Increases heart rate and force of contraction
• Relaxes GI muscle
β2
Gs-coupled (Adr>NA)
• Bronchodilation
• Vasodilatation in cardiac and smooth muscle
• Relaxation of uterine and bladder smooth muscle
• Muscle tremor (thermogenesis)
β3
Gi-coupled (NA≥Adr)
• Decreases heart rate and force of contraction
• Vasodilatation
• Relaxation of detrusor
A1
Gi-coupled
• Cardiac depression (similar to M2 activation)
• Bronchoconstriction in asthmatic subjects
• Presynaptic inhibition (reduce glutamate release in brain) - induces sleep and is an endogenous antiepileptic
A2
Gs-coupled - 2A/B 2A: • Vasodilation • Decreased activation of neutrophils 2B: • Vasodilation
A3
Gi or Gq-coupled
• Decrease eosinophil activation
P2X
Ionotropic (homo/heterotrimers) non-selective (allows calcium flux)
X1: mediate rapid phasic contraction of the vas deferens
X4: mediates ATP-mediated increases in force of contraction in the heart
P2Y
All GPCRs
H1
Gq-coupled
• Smooth muscle contraction in the bronchioles
• Blood vessel dilatation largely via NO
• Itching through activation of sensory nerves
H2
Gs-coupled
• Gastric acid secretion
• Increased heart rate