Essential Pharmacology
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steroid hormones are lipid
soluble
steroid hormones bind to
intracellular receptors
plasma membrane receptors 4 types
act as ion channels intrinsic enzymes activity interact with JAK kinases interact with G-proteins
GPCRs are coupled to
adenylyl cyclase phospholipase C directly to ion channels
GPCR coupled to ion channel produce …………. EPSPs and IPSPs
SLOW
Ionotropic plasma membrane receptors produce …….. EPSPs and IPSP
FAST
Calcium can act as a
second messenger
phospholipase C produces
DAG that regulated PKC and IP3 they regulated Ca2+
low EC50 indicated ………….affinity
high
how good the drug is at activating the receptor
efficacy
Clinical applications in the NMJ
paralysis (non or depolarising blockers) botulinum toxin anti-cholinesterases
muscarinic agonists
mimic the effects of the parasympathetic NS
muscarinic antagonists
block the effects of the parasympathetic NS