50. Receptors and Signalling Flashcards
what type of receptor is bound and activated by the neurotransmitters/hormones - adrenaline and noradrenaline
G protein coupled adrenoreceptors
alpha 1 is Ga….
activation of phosp….. …
Increase of I…. and D…
contraction of ?
Gaq
Phospholipid C
IP3 and DAG
vascular smooth muscle
alpha 2 Ga…
inhibition of ……
decrease of c…..
increase of ….. channels
decrease of …… channels
relaxation of the….
Inhibition of n……
Gai
adenylyl cyclase
cAMP
K+ channels
GI tract
noradrenaline
Beta 1 is Ga…
stimulation of aden…..
increase of c….
Increased
Gas
adenylyl cyclase
cAMP
Heart rate and cardiac muscle contraction
Beta 2 is Ga…
stimulation of aden…..
increase of c….
Dilation of the
Gas
adenylyl cyclase
cAMP
Bronchi
(also incr. HR but to a lesser extent than B1)
Beta 3 is Ga…
stimulation of aden…..
increase of c….
causes……
Gas
adenylyl cyclase
cAMP
Thermogenesis in skeletal muscle
what binds/activates B2 adrenoreceptors to cause bronchodilation for asthmatic patients
salbutamol
what binds/activates B1 and B2 adrenoreceptors to cause bronchodilation and has a massive side effect of Tachycardia
Isoprenaline
name some of Beta1 agonists
Noradrenaline
Adrenaline
Pindolol (partial )
name some of Beta2 agonists
Adrenaline
Noradrenaline
Salbutamol
Salmeterol
Pindolol (partial)
name 6 beta blockers (antagonists)
Bisoprolol
atenolol
propranol
metoprolol
carvedilol
sotalol
Receptors may be divided into 4 main ‘super-families’ or classes based upon their common structure and function?
name them.
Ligand gated ion channels
G protein coupled receptors
Kinase linked receptors
nuclear receptors
Give an example of a Ligand gated ion channel
Nicotinic acetylcholine receptor
Nicotinic acetylcholine receptor are permeable to what?
Na+, K+ and Ca2+
what do Nicotinic acetylcholine receptors do
Modulate fast synaptic excitation in the nervous system - excitatory post-synaptic potentials (EPSPs) and motor endplate potentials (EPPs). Also expressed on the post-ganglionic neuronal cell bodies in the autonomic nervous system
Drugs that act at as agonists at nicotinic acetylcholine receptors (nAChRs) are…?
acetylcholine
Nicotine
Varenicline (partial)
which drug is a phosphodiesterase inhibitor -> inndicated fro COPD
Theophylline
kinase linked receptors are
insulin receptors
kinase linked receptors are also called
enzyme coupled receptors
kinase linked receptors, when activated cause
parallel signaling cascades
Nuclear receptors are generally bound by….
steroid hormones
Nuclear receptors are ……….so are not …………. to the cell membrane
Intracellular…. Bound.
Nuclear receptors contain
DNA binding domains allowing for the control for gene transcription
what is the nuclear receptor structure
N-AF1-DBD-Hinge-LBD-AF2-C
AF-activation function site
DBD- DNA binding domain
LBD-Ligand binding domain
steroid hormones are ……… and pass through the plasma membrane to bind to nuclear receptors
Lipophillic
Drug Targets can be divided into 4 main categories:
- Receptors
- Enzymes
- Ion Channels
- Carrier Proteins
what is ibuprofen
a non steroidal anti inflammatory drug (NSAID) that acts at cyclooxygenase enzymes
how does ibuprofen work
It works by blocking enzymes in your body known as cyclooxygenase enzymes (COX-1 and COX-2).
These enzymes usually help produce substances called prostaglandins.
Prostaglandins are involved in causing pain, swelling, and inflammation by making blood vessels widen (vasodilation).
what side effects for taking ibuprofen
Irritation of the GI tract, possible impairment of renal function via inhibition of prostaglandin-evoked vasodilation.
what kind of drug is amlodipine
calcium channel blocker (antihypertensive)
when is amlodipine used
when a patient has angina and/or hypertension
how does amlodipine work
Calcium channel blocker so is an antagonist at Cav1.3 however slow association and long duration of action
what are SSRIs and what are they commonly used to treat
SSRIs stand for Selective Serotonin Reuptake Inhibitors. They are a class of drugs commonly used to treat depression and anxiety disorders.
what is SERT
Serotonin Transporter. It’s a protein that plays a crucial role in the brain’s serotonin system.
what is the function of SERT
is responsible for transporting serotonin, a neurotransmitter, from the space between nerve cells (the synaptic cleft) back into the nerve cell that released it (the presynaptic neuron).
This process is known as serotonin reuptake.
so what is the role in SSRIs in reducing depression
SSRIs (Selective Serotonin Reuptake Inhibitors) work by blocking SERT. This inhibition increases the amount of serotonin available in the synaptic cleft, which can help improve mood and reduce anxiety
name some drugs that act as SSRIs (antagonists at SERT)
Citalopram
Escitalopram
Fluoxetine
Fluvoxamine
Paroxetine
Sertraline
Sodium Valproate is used to treat who?
Epileptic people
Sodium Valproate has many what….
mechanisms of action
