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12 Cards in this Set
- Front
- Back
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Gi/Gs/Gq?
M1,M3,M5 |
Gq,increase PLC,IP3,DAG
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Gi/Gs/Gq
M2,M4 |
Gi, decrease cAMP
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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 |
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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 |
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what are heterorecetors?
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heteroreceptors: located on SN terminals. Activation: inhibits NE release. Mixture of M2 and non M2
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M3 selectivity
functions in organs |
M3: gland/sm
sm: increase contraction ( GI, airway, bladder, uterus, eye) sweat gland salivary secretion reduce food intake |
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M5 functions
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M5: involved in addiction
mediates ACH-induced dilation of cerebral arteries and arterioles |
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cholinergic agonists with no niconitic action
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methacholine, pilocarpin/muscurine, bethanechol
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2 main groups of directly acting cholinomimetics
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choline esters and natural /syntheti alkaloids
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alkaloid cholinergic agonist durgs and their structure
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Muscurine: 4 ammonium
pilocarpine : tertiary amine |
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choline esters
absorption BBB metabolism |
choline ester
hydrophilic poorly absorbed in GI can't cross BBB metabolized by ACHE |
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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 |
