Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
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 |