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