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Receptor enzymes
Receptor Transmembrane Intracellular or
● Guanylate cyclase
transmembrane
○ GTP -> cGMP -> activate PKG or CGMP dependent kinase
○ Atrial natriuretic peptide (ANP) : increase blood pressure = stretching = dec bv
Effects Rapid Slower or rapid
● Tyrosine Kinase
Peptide Hormones (hydrophilic) ○ Phosphorylation of tyrosine (autophosphorylation)
● Rough ER ○ Ras proteins: mutation; phosphorylates = inc production of substances =
● Preprohormones -> cleavage -> prohormone (vesicle) -> enzyme breakdown -> overamplification
active form ● Serine/Threonine Kinase
● Arginine-Vasopressin (fluid balance) ○ Direct phosphorylation of serine/threonine
○ Preprovasopressin (SP + AVP + neurophysin + glycoprotein) ○ TGF beta = like ras where overamplification
○ SP cleaved in RER = provasopressin
○ Cleavage in GA = AVP, NPH, GP
Steroid hormones (hydrophobic) Second Synthesized Action Effects
Messengers by the
● Synthesized in Smooth ER or mitochondria enzyme
● 3 classes: Mineralocorticoids, Glucocorticoids, Reproductive Hormones
● Cholesterol + desmolase -> pregnenolone -> progesterone
Ca2+ None Binds to Alters enzyme
○ 17-alpha hydroxylase = cortisol & sex hormone (testosterone, estrogen) calmodulin activity
○ 21-hydroxylase = aldosterone (sodium goes, water goes)
Amine Hormones
cGMP Guanylate Activates Phosphorylates
● Hydrophilic except thyroid hormones cyclase protein kinases proteins
● ACh, catecholamines (dopamine, nore, epinephrine), serotonin, melatonin, (usually protein
histamine, thyroid hormones kinase G) Opens and closes
● Cytokines are synthesized on demand ion channels
● Tyrosine (thyroid & catecholamines)
● Tryptophan (serotonin & melatonin) cAMP Adenylate Activates Phosphorylates
● Histidine (histamine) cyclase protein kinases proteins
Eicosanoids (hydrophobic) (usually protein
kinase A) Opens and closes
● Act as paracrines
ion channels
● Inflammation & pain: leukotrienes & prostaglandins
● Arachidonic acid (20C)
Phosphatidyl Phospholipase Activates Alters enzyme
○ COX (cyclooxygenase)
inositol C protein kinases activity
■ Prostaglandins, prostacyclines, thromboxanes C
■ Pain Phosphorylates
■ Celecoxib- inhibits COX = no pain Stimulates proteins
○ LOX (lipooxygenase) Ca2+ release
■ Leukotrienes from
intracellular
■ Inflammation
stores
● NSAIDS: ibuprofen, paracetamol, naproxen; inhibit COX/LOX
Amino acids
Cholinergic Receptors (acetylcholine) Summary: Phases of Action Potential
Receptor Location Effect of 2nd Agonists Antagoni AP Phase Na+ Na+ K+ K+ Membrane
subtype binding messeng sts Channel flow Channel Flow Potential
er
pathway Depolarization open Influx closed none – to -
(ecf ->
Nicotinic Neuromu Excitation Ion influx ACh, Curare icf)
(synapse scular nicotine,
s) junctions, carbachol Overshoot (peak open influx closed none 0 to +
ganglioni of action
c potential)
neurons,
adrenal
Repolarization closed none open efflux + to -
medulla
Hyperpolarization closed none open efflux - to –
Muscarini Gut Excitation G-protein Ach, Atropine,
c coupled muscarin scopolam
e, ine
carbachol Summary: Refractory Period
Sweat Activation Sodium channel gates Closed activation and Closed inactivation
glands inactivation gates gate or resting
Receptor Location (in Effect (in 2nd Sensitivity Graded potential Action Potential
subtype humans) humans) messenger
system Location of event Dendrites and cell Axon hillock
body
α1 Blood Vasoconstric G protein NE > E
vessels of tion activates Distance Traveled short Long distance - all
skin, gut, phospholipa throughout the length
kidneys, se C of axon
salivary
glands Amplitude Various (graded) and Constant (100 mV)
decremental
Α2 Membrane Inhibits G protein NE > E
(inhibitory) of release of inactivates Stimulus for opening of Chemical Voltage regulated
adrenergic NE adenylate ion channels (neurotransmitter) or
axon cyclase, sensory stimulus
terminals inhibits
cAMP Positive feedback cycle absent present
production (propagation)
Number of neurons in 2 2
chain
Location of cell bodies Thoracic & lumbar regions Hindbrain; sacral region of
of spinal cord spinal cord