Lectures 1-5 Flashcards
AChR’s - nicotinic agonist and antagonist?
Nicotine agonist
Curare antagonist
AChR’s - muscarinic antagonist
Atropine
Where is the first neurone in the SNS?
spinal chord ganglia
where is the first neurone in the PNS
cranium
How many parts does the AChR have?
5
What is the secondary neurotransmitter for the SNS?
noradrenaline
What does the mass action law tell us?
The concentration of the ligand receptor complex over time
What does radioligand binding assay measure?
The radioactivity of a ligand is used to measure the concentration when bound to a receptor
What do ligand gated ion channels cause?
depolarisation of the membrane
What type of receptors are ligand gated ion channels?io
ionotropic
What kind of receptors are GCPR’s?
metabotropic
What allows the G protein subunits to reassemble?
The hydrolysis of GTP in the alpha subunit
What does G alpha S do?
activates adenyl cyclase
what does G alpha i do?
deactivates adenyl cyclase
What does Gq do?
stimulates Phospholipase C
What does PIP3 do?
splits into insP3 and DAG
Explain the interaction between cAMP and PKA
cAMP binds to the regulatory subunits of PKA, releasing the catalytic subunits
They then phosphorylate target proteins and enter the nucleus, they phosphorylate CREB, which then recruits a CREB binding protein
The complex the activates transcription
What do kinase-linked receptors do?
phosphorylation of proteins
In the hypothalamus, what secretes TRH?
neurones
where to ductless endocrine glands secrete?
directly into the body
What is TRH
thyrotropin releasing hormone
What is TSH and where is it secreted?
thyroid stimulating hormone
secreted in the anterior pituitary
how are protein hormones formed from their precursors
proteolysis
What are corticotrophs
basophilic cells in the anterior pituitary which produce pre-pro-opiomelanocortins, which produce an ACTH
What is ACTH?
adenocorticotropic hormone
What is ACTH produced from?
corticotrophs - pre-pro-opiomelanocotrtins
How does cholesterol reach the mitochondria
steroid acute regulatory hormone (StAR)
Generally, where are steroid hormones produced?
adrenal cortex
What are the 5 groups of steroid hormones?
Glucocorticoids Mineralocorticoids Androgens Estrogens Progestogens
Are amine hormones lipophilic or lipophobic?
lipophilic
What is T4?
thyroxine - inactive precursor to T3
How are hyrdophobic hormones carried in the blood?
carrier proteins
expand on the term ‘ligand-inducible transcription factors’
steroid hormone bind to specific hormone response elements (HRE’s) in promotor regions, the TF’s are hence the receptors they bind to
What is K(D)?
concentration of the drug resulting in half of the available receptors being occupied
What are Ca2+ channels blocked by?
nifedipine
What is a super agonist?
an agonist which doesn’t have to bind to all the receptors to give maximal efficacy
Name 4 types of drug receptors
enzymes
ion channels
transporters
physiological receptors
What are dirty drugs?
drugs with many targets
When do nicotinic ACh receptors become visible?
They are low affinity, so only when the higher affinity muscarinic receptors become poisoned
What does atropine do?
lowers blood pressure
Name the 5 receptor super families
Integral ion channels Integral tyrosine kinases steroid (nuclear receptors) GCPR's Cytokines
