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29 Cards in this Set
- Front
- Back
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Inhibitory amino acids (NT)
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glycine
GABA |
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excitatory amino acids (NT)
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glutamate
aspartate |
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NMDA receptors bind to ______
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bind to glutamate (excitatory)
increases Ca2+ (also K+, and Na+) has a Mg2+ plug -removed by cell depolarization (AMPA rec.) |
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AMPA receptors bind to _______
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bind to glutamate (excitatory)
-multi-cationic channel -generally primary depolarizer of glutamate-responding cells -then move on to NMDA rec. |
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Nicotinic Receptor Types
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N1 = (para)sympathetic ganglia
N2 = neuromuscular junction |
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Nicotinic receptor structure and function:
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2x Ach [=] Nicotinic Receptor
increases Na+ conductivity (depolarizes) *binding to alpha-SU* |
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GABAa Receptor
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2x GABA [=] GABAa
increases permeability of Cl- (hyperpolarizes) allosteric activators = EtOH, barbituates, propofol, benzodiazepams |
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Benzodiazepams
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allosteric activators of GABAa
increase Cl- conductance hyperpolarize |
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EtOH
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allosteric activators of GABAa
increase Cl- conductance hyperpolarize |
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Propofol
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allosteric activators of GABAa
increase Cl- conductance hyperpolarize |
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Barbituates
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allosteric activators of GABAa
increase Cl- conductance hyperpolarize |
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Serotonin and 5-HT3 Receptors
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increase conductance of Na+
depolarize |
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Beta-GPCRs fxn
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increase cAMP
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GABAb receptors
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hyperpolarization
inhibits Ca2+ or increase K+ prevent release of glutamate from pre-synaptic neuron |
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Theophylline
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bronchodialator (not used anymore)
Adv.Eff>= seizures, fatal arythmias (-) phosphodiesterase prevent breakdown of cAMP ---> 5'-AMP |
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Caffeine
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relax sm. muscle of bronchioles
(-) phosphodiesterase prevent breakdown of cAMP ---> 5'-AMP |
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Papaverine
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(-) phosphodiesterase
prevent breakdown of cAMP ---> 5'-AMP |
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Effects of GPCR IP3 and DAG
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contraction of smooth muscle
increased glandular secretion |
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EGF Receptor Fxn
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Epidermal Growth Factor = EGF
Tyrosine Kinase---> transcription factor slower to act |
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Cortisol MOA Intracellular
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(cytoplasmic)
Cortisol [=] Cytoplasmic Gucocorticoid Rec --->dissociation of Heat-SHock Protein allows uncovering of DNA-binding site -->transcription factor -increase cytokines decrease lipocortin |
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MOA Estrogen, Androgens, Thyroxines
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transcription factors
steroids |
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Targets of phosphorylation in TK
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serine
threonine |
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IP3 and smooth muscle contraction
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activates MLCK
--------> +(P) to myosin light-chain (MLC) ----> MLC binds to actin ----> smooth muscle contraction EXCEPTION beta-2 VASODIALATION |
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IP3 and increased glandular secretion
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IP3 releases Ca++ from SER
-----> increased cytosolic Ca++ ---------> Ca++ [=] Calmodulin ---------> activated enzymes ---------> increased secretion |
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Beta-2 GPCR
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endothelial cells (vasodialation)
IP3-----> +(P) MLCK inactivates MLCK(P)----> no +(P) of MLC MLC cannot interact with actin ------------> no vascular contraction ----------> VASODILATION |
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Atrial Naturetic Factor MOA
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hit transmembrane GUANYLATE CYCLASE
--------> increase cGMP ----------> -(P) protein kinases (inactive) -----------> -(P) MLC --------------> VASODILATION |
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NO (nitric oxide) MOA
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hit transmembrane GUANYLATE CYCLASE
--------> increase cGMP ----------> -(P) protein kinases (inactive) -----------> -(P) MLC --------------> VASODILATION decrease platelet aggragates |
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NO (nitric oxide) produced by
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endothelial cells, neurons = constitutive
macrophages, neutrophils, sm. muscle cells = cytokine induced |
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Sildenafil
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inhibits phosphodiesterase of
cGMP----->5'GMP increases vasodilation, erection, and prevents platelet aggregation |
