Pharmacology Flashcards
what is the chemical name for aspirin?
acetylsalicylic acid
what substrate does the enzyme cyclooxygenase bind to?
long fatty acid chain, Arachidonic acid
adrenoceptors Bind to…
adrenaline and noradrenaline
True of False
most drugs bind reversibly to their receptors
True - ligand binding is governed by kinetics of association and dissociation.
what is Ec5o?
the effective concentration of ligand producing 50% of Emax maximal response.
what is potency?
ligand affinity + Efficacy
measure of a drug activity expresses in terms of amount required to produce an effect of a given intensity.
what is Efficacy?
how well as ligand-receptor complex causes a desired response.
what is radioligand binding?
allows quantification of ligand receptor affinity.
what is Bmax and Kd
Bmax - maximum binding capacity
Kd- dissociation constant - measure of ligand affinity
True or false
antagonists possess affinity and Efficacy (intrinsic Efficacy).
False
they possess affinity but lack intrinsic Efficacy.
what is the effect of presence of fixed concentration of competitive antagonists on concentration response curve?
rightward shift
what is signal transduction?
process by which a biological cell converts one kind of signal or stimulus into another.
what is a signalling scaffold?
the number of signalling molecules brought together in one place in the cell to communicate signalling from outside the cell to inside of the cell.
examples of therapeutic applications of drugs targeting GPCRs
depression, schizophrenia, acid reflux, nausea, hypertension, overactive bladder, asthma, chronic pain, glaucoma.
anti asthma drugs
beta adrenoceptor agonists
e.g salbutamol and salmeterol
analgesia/anaesthesia drugs
miu (u) opioid receptor agonists
e.g morphine and fentanyl
cardiovascular drugs
beta adrenoceptor antagonists
e.g propranolol and atenolol
neuroleptic drugs
D2 dopamine receptor antagonists
e.g Haloperidol and sulpiride
structure of GPCRs
single polypeptide chain
7 TM regions
extracellular Na terminal
intracellular C terminal
what are G proteins made up of?
1 alpha, 1 beta and 1 gamma subunits
what is the enzymatic activity /action of phospholipipase C?
converts PIP2 (phosphatidyl inositol phosphate 2) into 》 IP3 (Inositol 1,4,5 triphosphate) + DAG (diacyl glycerol)
stimulation of adenyl cyclamen leads to…
production of cyclic AMP, which leads to increased protein kinase A (PKA) activity.
Gas (G alpha s) coupled receptor
beta adrenoceptors
D1 dopamine receptors
H2 histamine receptors
inhibition of adenylyl cyclase leads to…
Gai (G alpha i) coupled receptors interact with and inhibit adenylyl cyclase, therefore no ATP is produced and PKA activity is reduced.
alpha 2 adrenoceptors
D2 dopamine receptor
miu opioid receptor
