Drugs and receptors Flashcards
what is a receptor
part of a cell that interacts with a specific ligand and initiates a change of biochemical events leading to ligand observable effects
what classes of chemicals can receptors communicate with
Neurotransmitters
Autacoids
Hormones
What type of receptors are there
Ligand gated ion channels
G protein-coupled receptors
Kinase linked receptors
Cytosolic/nuclear receptors
What are G protein-coupled receptor? (GPCR)
Family of proteins involved in transmitting signals from GPCR’s
what binds to and hydrolised GTP and GDP (guanine triphosphate + Guanine diphosphate
G proteins (gioamome. nucleotide-binding-proteins)
what is a kinase
Enzymes that catalyse the transfer of phosphate groups
What is a nuclear receptor and how do they worl
Steroid hormone receptors
Worryk by modifying gene transcription
has zinc fingers that bind to DNA
what type of cancer is tamoxifen used
Estrogen receptor+ cancers
give an example where an inbalance in chemicals can lead to a pathology
Allergy –> inc histamine
Parkinsons –> reduced histamine
Give and example where an imbalance in receptor can lead to a pathology
Myasthenia gravis – loss of ACh receptors
Mastocytosis –> increased c-kit receptor
What is an agonist
a compound that binds to a receptor and activated it
what is an antagonist
- A compound that reduces the effect of an agonist
- Affinity but not efficacy
give the equation for intrinsic activity
intrinsic activity = Emax of partial agonist / Emax of full agonist
What does intrinsic activity mean
the ability of a drug-receptor complex to produce a maximum function response
what is selective agonism
potency of a range of agonists