Test 2 Receptors Flashcards
α1 receptors
Increased vascular smooth muscle contraction via Ca2+ release.
Positively coupled to phospholipase C via Gq/11α and DAG. (increased IP3/DAG)
IP3 –> Ca2+ release from SR –> intracellular Ca2+ –> CaM –> MLCK activation –> phos of myosyin –> contraction
13-13
α2 receptors
pre-synaptic α2 receptor activation decreases neurotransmitter release via inhibition of adenylyl cyclase.
Decreased adenylyl cyclase –> decreased cAMP –> decreased PKA –> decreased phos of N-type Ca2+ channels –> reduced Ca2+ influx during AP –> decreased release of NT
Low PKA –> activation of MLCK –> vascular smooth muscle constriction (PKA phosphorylates MLCK and turns it off)
β1 receptors
Cardiac pacemaker cells - positively coupled to adenylyl cyclase via Gαs
increased adenylyl –> increase cAMP –> increased PKA –>
ionotropy: –> increased phosporylation of L-type Ca2+ channels –> greater Ca2+ influx and larger trigger for SR release, and increased SR Ca2+ for next release.
chronotropy: –> increased phos of Ca2+ channels –> increased Ca2+ inward current –> decreased threshold/faster nodal cell depolarization
β2 receptors
Regulates airway constriction and peripheral vascular resistance. Smooth muscle relaxation.
Positively coupled to adenylyl cyclase via Gαs.
Increased adenylyl cyclase –> increased cAMP –> increased PKA –> phosphorylation and inhibition/deactivation of MLCK –> reduction in affinitely for CaM –> reduced smooth muscle activity and relaxation.
M1
Activates myenteric plexus. Increases IP3, DAG, and Ca2+.
Muscarinic
M2
Opens K+ channels –> decreased HR and contraction (lowers CO)
Decreases cAMP, Ca2+ –> inhibits NE release from sympathetic nerve terminals
Muscarinic
M3
Increased IP3, DAG, and Ca2+ –> contracts circular ciliary musc (constriction of the pupil), bronchiolar muscle, GI smooth muscle, and bladder detrusor muscle.
Stimulates GI secretions, eccrine sweat glands, tear glands, and salivary glands.
Muscarinic
Nn
Neuronal nicotinic receptor. Na+/K+ channel. Binds Ach.
Ligand-gated ion channel - 5 subunits, four types. The two α types bind ligand.
Nm
Muscle nicotinic receptor. Na+/K+ channel. Binds Ach.
Ligand-gated ion channel - 5 subunits, four types. The two α types bind ligand.