Receptors Flashcards
What is the active ingredient of opium?
Morphine
How many types of opiate receptors are there?
3
Which drugs bind to the mu (μ) opiate receptor? (4)
- Morphine
- Heroin
- Codeine
- Fentanyl
What are the endogenous ligands for opiate receptors? (2)
- Endorphins
- Enkephalins
What is a drug?
A chemical of known structure which produces a biological effect when administered to a living organism
What is a biopharmaceutical?
A drug made from DNA (proteins, oligonucleotides, antibodies)
What is a medicine?
A chemical preparation that contains a drug(s) which is administered to produce a therapeutic effect
What are the 2 types of biologics?
- First generation
- Second generation
What are first generation biologics?
Copies of endogenous proteins produced by recombinant DNA technology
What are second generation biologics?
Engineered proteins to improve their performance e.g. humanised monoclonal antibodies
What are the 4 main classes of proteins targeted by drugs?
- Receptors
- Enzymes
- Transporters
- Ion channels
What happens if you increase the dose of drug too much?
Starts to have off-target side effects, toxicity etc.
What is an agonist?
A drug which switches on a receptor when it binds and brings about change in a cell
What is an inverse agonist?
- A drug which binds to the same site as an agonist but reduces receptor activity (opposite response to the agonist)
- Reduces its basal, constitutive activity
What is an antagonist?
- Blocks the activity of the receptor when it binds
- Stops the effect of an agonist/inverse agonist
What kind of receptors are opiate receptors?
G protein coupled
How does lidocaine work?
Blocks voltage gated Na+ channels for analgesia
What is a prodrug?
A drug which is processed by an enzyme to produce an active version of the drug e.g. L-dopa
What is the treatment for opioid overdose?
Naloxone
What are the 4 classes of receptors?
- Ligand gated ion channels (ionotropic)
- G-protein coupled receptors (metabotropic)
- Kinase-linked receptors
- Nuclear receptors
What is the structure of ionotropic receptors? (2)
- Subunits have a few transmembrane domains
- Multiple subunits come together to form the channel
What is the structure of metabotropic receptors? (2)
- 7 transmembrane domains
- Coupled to a G protein
What do kinases do?
Phosphorylate other proteins
Where are nuclear receptors found in a cell?
Cytosol or nucleus