Endocrine Pharmacology Flashcards
Thromboxanes, prostaglandins and leukotrienes are derived from?
Arachidonic acid
Dopamine, noradrenaline, and adrenalin are classified as?
Catecholamines
Is nitric oxide a hormone?
Yes
Receptors to which molecules are ligand-gated ion channels?
Receptors to GABA, Ach, ATP and glutamate
Receptors to which molecules are G-protein coupled receptors?
PTH, oxytocin, somatostatin, catecholamine
Receptors to which molecules are enzyme-linked receptors?
Insulin, cytokines
Receptors to which hormones are classified as nuclear receptors?
Steroid hormones, thyroid hormones, vitamin D
Ion channels change the
Membrane potential of the cell
Ligand gated ion channels are
Ionotropic receptors
Ligand gated ion channels have an immediate
Effect
G- protein coupled receptors are
Metabotropic receptors
Examples of metabotropic receptors are
Muscarinic and Ach receptor
Kinase-linked receptors take how long to induce its effects?
Hours
What is an example of a kinase-linked receptor?
Cytokine receptor
Nuclear receptors take how long to induce its effect?
Hours
An example of a nuclear receptor is?
Oestrogen receptor
What does Gas do?
Stimulates adenylyl cyclase, causing increased cAMP formation
What does Gai do?
Inhibits adenylyl cyclase formation decreasing cAMP formation
What does Gaq do?
Activates phospholipase C increasing production of second messengers inositol triphosphate and diacylglycerol
What are some parts of the nuclear receptor?
N-terminus AF1 Co-activator region/Core DNA binding domain with ‘zinc fingers’ / Hinge region/ Ligand-binding domain AF2 Co-activator region HSP binding/ C terminal extension
What are some characteristics of the Class 1 nuclear receptors?
Present in the cytoplasm, operate as homodimers, mainly endocrine ligands, high affinity
What are some characteristics of the hybrid class of nuclear receptors?
Mainly endocrine/operate as RXR heterodimers
What are some characteristics of class 3 nuclear receptors?
Present in nucleus/operate as heterodimers/ mainly lipid ligands/low affinity
Glucocorticoid receptors are an example of which class of nuclear receptor?
Class I