ANS Receptors and Drug Targets Flashcards
M1 receptor mechanism
Gq protein - STIMULATORY
activate PLC –> convert PIP2 –> IP3 + DAG –> increase Ca2+
M1 receptor locations
brain, salivary glands
M1 receptor effects
increase secretions
M2 receptor mechanism
Gi protein - INHIBITORY
inhibit AC –> decrease cAMP
M2 receptor locations
heart
lugns
smooth muscle
presynaptic neurons
M2 receptor effects
decrease HR/contractility
bronchoconstriction
smooth muscle contraction
autoinhibition of synapses
M3 receptor mechanism
Gq protein - STIMULATORY
activate PLC –> convert PIP2 –> IP3 + DAG –> increase Ca2+
M3 receptor locations
pupils
detrusor muscle
lungs
M3 receptor effects
miosis
detrusor contraction –> urine release
bronchoconstriction
a1 receptor mechanism
Gq protein - STIMULATORY
activate PLC –> convert PIP2 –> IP3 + DAG –> increase Ca2+
a1 receptor locations
blood vessels
pupils
smooth muscle
internal urethral sphincter
CNS
a1 receptor effects
vasoconstriction
hypertension
mydriasis
smooth muscle contraction
internal urethral sphincter contration –> urinary retention
increased alertness/excitement
a2 receptor mechanism
Gi protein - INHIBITORY
inhibit AC –> decrease cAMP
a2 receptor locations
presynaptic neurons
CNS (locus coeruleus)
heart
blood vessels
endocrine
a2 receptor effects
autoinhibition of synapses
a2 agonists:
sedation, amnesia, analgesia, muscle relaxation
decrease HR
high dose: vasoconstriction/hypertension
low dose: vasodilation/hypotension
inhibit ADH –> increased urination
inhibit insulin –> hyperglycemia
B receptor mechanism
Gs protein - STIMULATORY
stimulate AC –> increase cAMP