Notes in PHAR212 L2

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Published	01/29/2024	Binding = ({{c1::the total number of receptor sites}} x {{c1::concentration of drug}}) / ({{c2::concentration of drug}} + {{c2::equilibrium dissociati…
Published	01/29/2024	The ligand must be {{c1::tranduced}} into the cell's machinery to produce a physiological response AKA {{c1::coupling}} or {{c1::signal transduction}}
Published	01/29/2024	Spare Receptorsthere is an {{c1::unequal}} proportion or ratio between {{c1::receptors and effectors in either time or space}}serves to make drugs muc…
Published	01/29/2024	Spatialy Sparewhen {{c1::100% response}} is elicited by {{c1::less than full receptor occupancy}}{{c1::maximum response}} using {{c1::anything but 100…
Published	01/29/2024	Consider “Cell A” with 1:1 ratio of receptors to effectors (4 of each) At C = KD results in 50% response, since 50% of effectors are activated. Recept…
Published	01/29/2024	In “Cell B,” receptors are increased 10x but effectors remain the same. Two effectors (resulting in 50% response) are activated at C << KD.Are t…
Published	01/29/2024	What is Temporally Spare?
Published	01/29/2024	Why do receptors decrease their sensitivity to agonists over time? (3)
Published	01/29/2024	What is Receptor Desensitization? How long does it last?What is its mechanism?
Published	01/29/2024	What is Receptor Down-Regulation?
Published	01/29/2024	What are the causes receptor down-regulation?
Published	01/29/2024	What is Supersensitivity?
Published	01/29/2024	What is tachyphylaxis?
Published	01/29/2024	What is Hypersensitivity?
Published	01/29/2024	What is an idiosyncratic reaction?
Published	01/29/2024	What is synergy?
Published	01/29/2024	What are the steps for Transmembrane Signalling Mechanism?Lipid-soluble chemical {{c1::crosses membrane to activate intracellular receptor.}}Binding t…
Published	01/29/2024	Lipid Crossing is the {{c1::first}} step of transmembrane signallingIt requires a {{c1::lag period}} of 30 minutes to several hoursIts effects are {{c…
Published	01/30/2024	The second step to transmembrane signaling mechanism is the {{c1::binding to the extracellular domain of transmembrane protein activates an intra…
Published	01/30/2024	Ligand-Regulated EnzymesBinding of Ligand (epidermal growth factor) to receptor{{c1::exposes tyrosine sites}}, {{c1::activates tyr-kinases}}, and {{c1…
Published	01/30/2024	Activation of JAK-STATBinding of cytokines to receptor leads to{{c1::dimer formation}} which activates {{c1::mobile}} (e.g. JAK) {{c1::kinase}}JAK pho…
Published	01/30/2024	Binding of ligand to extracellularly-facing sites creates {{c1::conformational shifts}} in subunit structureopens {{c1::aqueous channel allo…
Published	01/30/2024	G-protein Coupled Receptoragonist binding activates the receptor, leading to {{c1::GDP release}} and {{c1::binding of GTP to G-protein}…
Published	01/30/2024	GPCR is {{c1::serpentine}} and exists {{c1::intracellularly and extracellularly}}The G protein exists only {{c1::intracellularly}}
Published	01/30/2024	The Purpose of Second Messengers is to
Published	01/30/2024	Examples of Second Messengers
Published	01/30/2024	cAMPuses {{c1::Gs}} GTP binding protein{{c1::adenylate cyclase}} converts {{c1::ATP}} to form cAMPcomplex of {{c1::effectors}} comprised of regulatory…
Published	01/30/2024	Drugs with direct effects on {{c1::neurotransmission}} predominantly interact with two major types of receptors: {{c1::Metabotropic}} – drug interact…
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