C2 Structure Flashcards
what G protein coupled signaling results from what adrenoreceptors
a1 = Gq a2 = Gi/Go B1/B2/B3 = Gs
describe the events of B1 binding to cardiac muscle
B1 activate via Gs.
B1 –> adenylyl cyclase –> cAMP –> PKA
= In Ca influx = In force of contraction
describes events of B2binding to Smooth muscle
B2 activate via Gs.
B2 –> adenylyl cyclase –> cAMP –> PKA
= phosphorylation MLCK = Relaxation
describe the activation process of NA binding to a2
activates Gi/o: Ca influx –> smooth muscle contraction
describe the activation process of NA binding to a1
activates Gq –> PLC: PIP2 –> IP3 + DAG
IP3 = Ca efflux from ER & DAG –> PKC = smooth muscle contraction
name possible modifications of NA
removing OH –> dopamine (little activity @ adreno) = BetaOH essential
adding CH3 –> a-meNA: Increases selectivity & decreases potency @ a2
2y amines: Adr & Isoprenaline: Increases bulk amine substituent = decrease alpha activity/ Increase Beta activity.