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26 Cards in this Set

  • Front
  • Back
  • 3rd side (hint)
NE and EPI receptors
α1, α2, B
α1- Gq, PLC pathway

α2- Gi/o (ion channels, AC)

B- Gs (AC)
α1 antagonist
Prazosin
treats high BP, PTSD, anxiety
α1 agonist
Methoxamine
vasoconstriction, increases BP
α2 agonist
Guanfacine
hypertension and ADHD (PFC, LC)
α2 antagonist
Yohimbine
increases firing of LC neurons, helps with recall of memories in therapy sessions of PTSD patients
B agonist
Isoproterenol
to treat bradycardia
B antagonist
propanolol
to treat PTSD
Ionotropic receptors for Ach
nicotinic receptors

nAchR
neuromuscular junction
autonomic ganglia
adrenal medulla
CNS
Metabotropic receptors for Ach
muscarinic receptors

M1,3,5 (Gq, PLC)

M2,4 (Gi/o, M2 is autoreceptor, AC and acts to inhibit ion channels w/ Ca++ decrease due to GIRK K+ hyperpolarization)
located peripherally and throughout CNS
AChE inhibitors used to treat...
Alzheimer's
Sarin, soman, tabun
irreversible anticholinesterase compounds
curare
nictonic receptor antagonist (paralytic, NM junction)
nicotine
nicotinic receptor agonist
(smoking may decrease Alzheimer's risk by agonist use preventing degeneration of ACh neurons)
Belladonna
muscarinic antagonist
pupil dilator (with high doses get cognitive impairment, delirium, tachycardia, autonomic symptoms)
u receptors
regions associated with descending analgesic pathways (PAG, RVM, amygdala, dorsal horn)

reward regions (VTA and nucleus accumbens)

dorsal striatum and LC
endogenous ligand: B-endorphin

-morphine-like opiate drugs
6 receptors
dorsal horn, other brain regions
enkephalins
K receptors
dorsal horn, dorsal striatum, nucleus accumbens, deep cortical layers, others
dynorphin
opiod peptides made in what brain regions?
hypothal, striatum, hippo, amygdala, pituitary gland, medulla, others
opioid peptides
all start with try-gly-gly
ex. enkephalins, dynorphins, neoendorphins
neuropeptide packaging
into LDCVs (large dense0core vesicles)
neuropeptide release
need more ca entry for a longer period of time (sustained activity)

need long term stimulation of presynaptic cell (longer relative to classical NTs)
neuropeptide reuptake
NO REUPTAKE!
destruction of excess neuropeptide by catabolic peptidases, then have inactive metabolites
all opiate receptors are...
receptor--Gi--AC-- (-)
u ex.

GABA (-) --VTA (+) -- NAcc
opiates have long ranked among the most important drugs in the phramacopoeia because...
primarly bcause of their potent analgesic properities, but also becaues of their antitussive and antidiarrheal effects
Opiate examples
Heroin, Oxycodone, Morphine, Fentanyl, Codeine, Hydrocodone, Vicoprofen
Opium- poppy tears
Morphine, Codeine, Heroin
Codeine - 3-methylmorphine
-Prodrug, metabolized to produce morphine,
produces 5-10%, less potent and less addictive

Heroin- diacetylmorphine
orally-extensive 1st pass metabolism, prodrug for morphine

injected-avoids first pass metabolism, rapidly crosses BBB because of acetyl groups, metabolized to 6-MAM and 3-MAM and quicker acting and more addictive