autonomic/cns

• 1. Types:
• - a1-gq coupled: increases IP3 & Ca --> contracts arterioles

- a2-gi coupled: inhibits AC --> dec cAMP --> inc heart contraction

- b1/b2-gs coupled: activate AC --> inc cAMP --> relax bronchiole SM

- b2 more sensitive to E than to NE (higher affinity for E)

2. Endogenous ligands: E & NE

1. vasoconstrict arteries to heart, veins, & dec motility of GI SM

2. a1: SM contraction; a2: inhibit insulin release, activate sphinctors, activate thrombocyte agg.

- b1: inc HR/CO, inc contraction, inc renin secretion

- b2: SM relax, dilation (dec bp), inhibit His release from mast cells

- b3: inc lipolysis in adipose tissue

1. Catecholamines, Non-catecholamines

• 2.
• Catecholamines:
• - clonidine (a2 agonist)
• - dobutamine (b1 agonist)
• - isoproterenol (b2 agonist)
• - E & NE (non-selective)

• Non-catecholamines:
• - tetrahydrozoline / visine (a agonist)
• - phenylephrine (a1 agonist)
• - pseudoephedrine (a1 agonist)
• - albuterol (b2 agonist)

• 1. propanolol (dec HR, bp)
• 2. labetalol (also a1 antagonist)

• AChE inhibitor
• competitive antagonist

• bromocriptine
• amantadine
• L-DOPA + carbidopa = Sinemet

• a2 agonist
• catecholamine

• b agonist
• catecholamine

• non-selective agonist
• catecholamines

• b1 agonist
• catecholamine

• visine
• non-catecholamine
• a agonist --> constrict bvs to dec red eye

• a1 agonists
• non-catecholamines
• decongestant (vasoconstrictor --> dec perfusion rate)

• b2 agonist
• non-catecholamine
• treatment for asthma

• DA agonist
• parkinson's disease treatment
• longer 1/2 life but less effective than LDOPA

• inc DA release
• parkinson's disease treatment

• parkinson's treatment
• allows L-DOPA to cross BBB without being metabolized by AAAD (carbidopa inhibits AAAD enzyme)