Flashcards in Pharmacokinetics and Pharmacodynamics IV Deck (25)
What type of receptors are muscarinic ACh receptors?
G-protein coupled receptors that act through 2nd messengers (p.230)
What are the subtypes of muscarinic receptors?
M1, M2, M3, M4, M5 (p.230)
What are the receptor types for the sympathetic nervous system?
a1, a2, b1, b2 (p.231)
What type of G protein class is each sympathetic nervous system receptor composed of?
a1- q; a2- i; b1- s; b2-s (p.231)
What are the three principle functions of a1 sympathetic nervous system innervation?
Increased vascular smooth muscle contraction; increased pupillary dilator muscle contraction (mydriasis); increased intestinal and bladder sphincter contraction (p.231)
What are the four principle functions of a2 sympathetic nervous system innervation?
Decreased sympathetic outflow, decreased insulin release, decreased lipolysis, increased platelet aggregation (p.231)
What are the four principle functions of b1 sympathetic nervous system innervation?
Increased heart rate, increased contractility, increased renin release, increased lipolysis (p.231)
What are the nine principle functions of b2 sympathetic nervous system innervation?
Vasodilation, bronchodilation, increased heart rate, increased contractility, increased lipolysis, increased insulin release, decreased uterine tone (tocolysis), ciliary muscle relaxation, increased aqueous humor production (p.231)
What are the receptor subtypes for the parasympathetic nervous system?
M1, M2, M3 (p.231)
What type of G protein class is each parasympathetic nervous system receptor composed of?
M1- q; M2- i; M3- q (p.231)
Where are M1 receptors of the parasympathetic nervous system active?
CNS, enteric nervous system (p.231)
What are the two principle functions of M2 parasympathetic nervous system innervation?
Decreased heart rate, decreased contractility of atria (p.231)
What are the seven principle functions of M3 parasympathetic nervous system innervation?
Increased exocrine gland secretions (e.g. lacrimal, gastric acid), increased gut peristalsis, increased bladder contraction, bronchoconstriction, increased pupillary sphincter muscle contraction (miosis), ciliary muscle contraction (accomodation) (p.231)
Name the dopamine receptors and their respective G-protein linked 2nd messengers.
D1- s; D2- i (p.231)
What is the result of D1 receptor activation?
Relaxed renal vascular smooth muscle (p.231)
What is the result of D2 receptor activation?
Modulation of transmitter release, especially in the brain (p.231)
Name the histamine receptors and their respective G-protein linked 2nd messengers.
H1- q; H2- s (p.231)
What is the result of H1 receptor activation?
Increased nasal and bronchial mucous production, contraction of bronchioles, pruritus, pain (p.231)
What is the result of H2 receptor activation?
Increased gastric acid secretion (p.231)
Name the vasopressin receptors and their respective G-protein linked 2nd messengers.
V1-q; V2-s (p.231)
What is the result of V1 receptor activation?
Increased vascular smooth muscle contraction (p.231)
What is the result of V2 receptor activation?
Increased H2O permeability and reabsorption in the collecting tubules of the kidney (p.231)
Describe the Gq second messenger cascade.
Activation of PLC induces IP3 to produce DAG (produces protein kinase C) and IP3 (increases intracellular calcium and induces smooth muscle contraction) (p.231)
Describe the Gi second messenger cascade.
Inhibits adenylyl cyclase thereby decreasing cAMP and protein kinase A and myosin light chain kinase in smooth muscle (p.231)