G-protein coupled receptors
7 transmembrane domain associated with G-protein. G-protein has alpha, beta, gamma subunits. Alpha subunit bound to ATP. Once GPCR binds ligand, ATP cleaved releasing G protein to activate second messengers.
G-protein coupled receptors associated with Gq
G-protein coupled receptors associated with Gs
G-protein coupled receptors associated with Gi
Cyclic GMP second messenger system
Gi second messenger system
Ligand binds to R–> Gi activation–> decreases AC activity–> ATP not converted into cAMP–> cAMP does not activate PKA–> PKA does not inactivate MLCK allowing for myosin phosphorylation and smooth muscle contraction. PKA does not increase intracellular calcium in heart muscle.
Gs second messenger system
Ligand binds to R–> Gs activation–> increases adenylyl cyclase–> turns ATP into cAMP–> cAMP activates Protein Kinase A (PKA). PKA increases intracellular calcium concentrations in the heart. PKA decreases intracellular calcium concentrations in smooth muscle (eg, bronchioles) and inhibits myosin light-chain kinase (thus inhibiting myosin phosphorylation and smooth muscle cell contraction contraction).
Gq second messenger system
Ligand binds to R–>Gq activation–>Phospholipase C–> breaks up lipid membrane PIP2 into DAG and IP3. DAG–> Protein Kinase C (PKC). IP3–> liberates intracellular Ca2+ from endoplasmic reticulum–> smooth muscle contraction.
Alpha 1 receptor
Alpha 2 receptor
Beta 1 receptor
Beta 2 receptor
Beta 3 receptor
M1 receptor (muscarininc AChR)
M2 receptor (muscarininc AChR)
M3 receptor (muscarininc AChR)
D1 (dopamine) receptor
D2 (dopamine) receptor
H1 (histamine) receptor
H2 (histamine) receptor
V1 (vasopressin) receptor
V2 (vasopressin) receptor