Receptor Theory (Owen) Flashcards
How do most drugs work?
By interacting with endogenous proteins.
What can drugs do to endogenous proteins?
Antagonize, block, or inhibit endogenous proteins.
Activate endogenous proteins.
What is pharmacology?
The study of what drugs do and how they do it. This includes interactions between drugs and body constituents at any level of organization.
A knowledge of pharmacology is essential for using drugs ______ and ______as therapy
…..safely…..effectively…..
What is a drug?
Any chemical compound that may be used on or administered to humans or animals as an aid in the diagnosis, treatment, or prevention of disease or other abnormal condition for the relief of pain or suffering, or to control/improve any physiological pathological condition.
How do drugs bring about change in biological functions?
Through their chemical actions.
What is a receptor, in terms of pharmacology?
A macromolecular component of the organism that binds the drug and initiates the drug’s effect.
Describe what you’d expect to find as a receptor.
Proteins that have undergone various post-translational modifications such as covalent attachments of carbohydrates, lipids, and phosphates.
How do some drugs antagonize, block, or inhibit endogenous proteins?
They act as: Antagonists of cell surface receptors Antagonists of nuclear receptors Enzyme inhibitors Ion channel blockers Transport inhibitors Inhibitors of signal transduction proteins
Why do cell surface receptors exist?
To transmit chemical signals from the outside to the inside of the cell.
What is a receptor antagonist?
A drug that “antagonizes” or “blocks” the receptor.
How might a drug prevent a response involving cell surface receptors?
The drug can bind the cell surface receptor without activating a receptor to trigger a response. It can also, by virtue of binding, prevent the endogenous chemical from binding the receptor, also preventing it from triggering a response.
What kind of cell surface receptor drug is used for angina, myocardial infarction, heart failure, high blood pressure, and performance anxiety?
Beta-adrenoreceptor blockers
How do beta-adrenoreceptor blockers work?
Via beta-blocking - they decrease the force of heart contractions so that the heart works less. Blocking the Beta1 by this Beta1Beta2 drug leads to less renin.
What is an example of a beta-adrenoreceptor blocker?
Propranolol
What is a nuclear receptor?
A receptor that exists in the intracellular compartment and upon activation binds to regulator regions in the DNA and modulates gene expression.
Some drugs bind to _____ _____, yet do not activate the receptors to translocate to the nucleus to bind _____ and alter _____ ______.
…..nuclear receptors…..DNA…..gene expresssion.
When nuclear receptors bind the drug molecule, the _____ ______ cannot bind to the receptor and thus cannot ______ ______ ______.
…..endogenous chemical…..alter gene expression.
What kind of nuclear receptor drug is used for prevention and treatment of breast cancer?
Estrogen receptor antagonists
What is an example of estrogen receptor antagonists?
Tamoxifen
How do drugs work by blocking ion channels?
Some drugs bind to ion channels and physically block cell membrane pores or cause an allosteric change that closes the pore.
Changes in the _____ concentration of ions mediate the effects of inhibitors of ion channels.
…..intracellular…..
What kind of drug that blocks ion channels is used for angina and high blood pressure?
Calcium channel blockers (CCBs)
What is an example of CCBs?
Diltiazem
