Principles drugs Flashcards
what is the effect of H1- histamine
what G protein
- smooth muscle contraction (increases iP3)
- Gq
what does B2- adrenoreceptor do and what G proteins
smooth muscle relaxation (increase cAMP). Gs and Gi
what does M2-muscaranic receptor do. and what G protein
decrease heart force of contraction (decrease cAMP) as more Gi than Gs so more AC inhibited than deactivated.
Gs and Gi
what does muscarinic M2 receptor do when soley Gi coupled. what g protein
cardiac slowing. gi protein
what does Gq generally do
activate phospholipase C, which activates second messenger iP3, releasing Ca2+ from intracellular cells and activating protein kinase C
how does Gs work
activate adenyl cyclase which converts ATP-> cAMP which activates protein kinase A
how does Gi work
inhibits adenyl cyclase so inhibits production of ATP to cAMP, therefore no/less protein kinase is produced
how does Gi wok in K+ channels in cell membrane
it increases opening of channels resulting in hyperpolarisation
what does loratidine do
what G protein
gq.antagonist of H1 histamine
what does adrenaline do
what g receptor
agaonist of B2 adrenoreceptor. gi and gs
what does salbutamol do
what g receptor
agonist of B2 adrenoreceptor. gi and gs
what does propanolol do
what g protein
antagonist of B2 adrenoreceptor
Gs and Gi
what does acetylcholine do and what g receptor
M2 agonist. gs and gi
what does atropine do
Muscaranic antagonist. gs and gi
what does acetylcholine do in cell membrane
m2 agonist . gi.so increases opening of K+ channels
wat does atropine do
antagonist of M2
what are the ligand gated ion channels
Nicotinic ACh receptor
GABAA receptor
glycine receptor
5HT3 receptor
glutamate receptors (NMDA)
what are the G protein coupled receptors
Muscarinic ACh receptors
Adreno-receptors
acetylcholine receptors
adrenoceptors
neuropeptide
hemokine receptors
protease activated receptors
what are the enzyme linked receptors types
Insulin receptor
serine/ threonine kinase
Cytokine receptor
what are examples of receptors that affect gene transcription
Steroid and thyroid hormone receptors
give examples of receptors linked to ion channels
ligand gated ion channels or iotrophic receptors
what are the receptors linked to ion channels
ligand gated ions or ioonotrophic receptors
what are the G couple protein receptos
metabotrophic receptors
what are the enzyme linked receptors
kinase
give an example of Gq receptor
prostanoid
give to examples of Gi protein couples receptos
opoid and cannabinoid
what G protein is cannabinoid receptor
Gi
what G protein is serotonin receptor
Gs
give two examples of Gs receptors
histamine and serotonin
what are the enzyme receptors
tyrosine kinase, serine/threonine and insuline receptor
what ae the GPCR receptors
thyroid stimulating hormone receptor
what are the intracellular receptors
nuclear/cytoplasmic, oestrogen receptor, vitamin D receptor. including steroid drugs and hormones, thyroid hormones, vitamins A and D, various lipids and xenobiotics
what receptors are .lipid soluble and which ones are water soluble
GPCR/enzyme receptor= water soluble
allintracellular inc steroids = lipid soluble
how does Gs work
– stimulates adenylyl cyclase, causing increased cAMP
how does Gi work
inhibits adenylyl cyclase, causing decreased cAMP
how does Gq work
activates phospholipase C, increasing production of second messengers inositol triphosphate and diacylglycerol
give an example of where G protein couples found and describe how it works
e.g. there are G protein-gated potassium channels in cardiac muscle which contributes to the regulation of heart rate (Ach released from vagus nerve binds to the G-protein coupled receptor which leads to opening of K channels
what are the 2 other names for G protein couples
metaboric or 7TDM
what does G protein coupled receptors structures combine
Structures comprise seven membrane-spanning 𝛼 helices, often linked as dimeric structures
what are 2 important receptors in enxyme linked receptors
MAP kinase pathway – important for cell division, growth and differentiation
JAK/STAT pathway – important for synthesis and release of inflammatory mediators
