ICPP session 6-12 Flashcards
GPCR action
- Ligand binds at binding domain
- Causes conformational change
- GDP dissociates from alpha subunit and is replaced by GTP
- beta-gamma unit and alpha subunit dissociate, alpha GTP activates effector protein (e.g adenylyl cyclase)
- Triggers conversion of ATP-> cyclic AMP, activates protein kinase A/ phospholipase C leads to conversion of PIP2 to IP3 and DAG, which activate protein kinase C
- GTP is hydrolysed to GDP on alpha subunit and subunits reassociate
Intracellular receptor binding
Hormone binds at hormone binding site, inhibitory protein complex dissociates exposing DNA binding site
G protein types
G alpha s: stimulates adenylyl cyclase
G alpha i: inhibits adenylyl cyclase
G alpha q: stimulates phospholipase C
Types of G protein coupled receptors
QISS QIQ
Alpha 1: alpha Q subunit, effects phospholipase C
Alpha 2: alpha I subunit, effects adenylyl cyclase
Beta 1: alpha S subunit, effects adenylyl cyclase (located in heart)
Beta 2: alpha S subunit, effects adenylyl cyclase (located in lungs)
M1: alpha Q subunit, effects phospholipase C
M2: alpha I subunit, effects adenylyl cyclase
M3: alpha Q subunit, effects phospholipase C
Branches of autonomic nervous system (origin + types of nerves)
Sympathetic: originates in lateral horn of thoracic and lumbar spinal cord, short preganglionic neurone, long postganglionic neurone, ganglia located in PARAVERTEBRAL CHAIN
Parasympathetic: originates in lateral horn of medulla and sacral spinal cord, long preganglionic neurone, short post, ganglia within INNERVATED TISSUES
Parasympathetic discharge pathological effects
Salivation- stimulation of salivary glands
Lacrimation- stimulation of lacrimal gland
Urination- relaxation of urethral internal sphincter muscle
Defection
GI upset- smooth muscle tone changes
Emesis- vomiting
Drug administration methods
OI IT IS SIR Oral Intravenous Intramuscular Transdermal Inhalation Sublingual Subdermal I? Rectal