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12 Cards in this Set

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Gi/Gs/Gq?
M1,M3,M5
Gq,increase PLC,IP3,DAG
Gi/Gs/Gq
M2,M4
Gi, decrease cAMP
M1 receptor, selective for what?
functions
selective-ganglionic
muscurinic effect in sympathetic ganglion, block K channel, stimulate SNS

increase secretory/motor activity of gut

involved in epilepsy
M2 receptor, selectivity
functions in organs

effect of increase ACH release
M2-cardio

stimulation of PSN, release of ACH from vagal, activate M2 on SN to reduce HR

smooth m

heteroreceptor. critical for analgesia, learning, memory

autoreceptor: presyn inhibition of ACH release at PSN terminal

stimulate contraction of airway sm and secretion from submucosal glands
what are heterorecetors?
heteroreceptors: located on SN terminals. Activation: inhibits NE release. Mixture of M2 and non M2
M3 selectivity
functions in organs
M3: gland/sm

sm: increase contraction ( GI, airway, bladder, uterus, eye)

sweat gland

salivary secretion

reduce food intake
M5 functions
M5: involved in addiction
mediates ACH-induced dilation of cerebral arteries and arterioles
cholinergic agonists with no niconitic action
methacholine, pilocarpin/muscurine, bethanechol
2 main groups of directly acting cholinomimetics
choline esters and natural /syntheti alkaloids
alkaloid cholinergic agonist durgs and their structure
Muscurine: 4 ammonium
pilocarpine : tertiary amine
choline esters

absorption
BBB
metabolism
choline ester
hydrophilic
poorly absorbed in GI
can't cross BBB

metabolized by ACHE
alkaloids

what class of drugs
absorption of pilocarpine/muscurine
metabolism
alkaloids

cholinergic agonist

pilocarpine : tertiary amine, well absorbed

muscurine: 4 amine, absorbed less in GI tract

excretion accelerated by acidification of urine

can cross BBB