________________ signaling is IONIC within cell, but could not use to jump from one
neuron to another - ANSWER-Electrical
(1)
Agonist:
Antagnoist: - ANSWER-Agonist: mimics action of neurotransmitter
Antagonist: blocks action of neurotransmitter
(1)
Dopamine Transporter has how many transmembrane domains? - ANSWER-12
(1)
Dose vs Dosage - ANSWER-Dose: Amount taken (10 mg)
Dosage: amount of drug/ body weight (concentration)
(1)
Electrical Signaling
,Maintains _______________ ___________________ --> difference in concentration of
ions between inside and outside (EX: pressure of water in hose) - ANSWER-Voltage
Potential
(1)
Excitatory:
Inhibitory:
Modulator: - ANSWER-Excitatory: Increase prob neuron will fire
Inhibitory: Decrease prob neuron firing
Modulator:
EX: Dopamine modules cell to make more likely to fire in certain situations and less
likely in others
(1)
Function of Nervous System: - ANSWER-1. Receive info from what's going on in
environment
2. Process info
3. Respond (execute some sort of action
(1)
What does the half-life tell us? - ANSWER-How long a drug stays in body (kidney
filtering out)
(1)
Steroid Hormone Receptors are where? - ANSWER-Not within membrane but INSIDE
cell
** has to dissolve in and get to the receptor which is in the cell
** Lipophillic
(1)
A cocaine receptor is which type? - ANSWER-Dopamine Transporter
(1)
ADME (pharmacokinetics) - ANSWER-Absorption
Distribution
Metabolism
Elimination
,(1)
Affinity:
Efficacy:
Toxicity:
Potency: - ANSWER-Affinity: Kd = how tightly drug binds to receptor (effects potency) --
> potency is measured by concentration of drug at 50% potency point ** where slope
changes
Efficacy: ED50 = effective dose
Toxicity: LD50 = lethal dose
Potency: Strength (KD + ED)
(1)
Biosynthesis and Catabolism of AMINES
How neurotransmitters generated? (with example of dopamine) - ANSWER-Tyrosine -->
Tyrosine Hydroxylase) --> L-Dopa --> Dopa Decarboxylase --> Dopamine --> Dopamine
B-hydroxylase --> NE
(1)
Clinical Trials
Investigational New Drug (IND)
- after animal research --> make it to FDA
Phase I:
Phase II:
Phase III:
PHase IV: - ANSWER-Phase I: SAFETY; small sample; take for first time every
Phase II: EFFECTIVENESS & SAFETY; small pop ask if doing what intended; give to
HEALTHY individuals (could recover)
Phase III: Efficacy & STANDARD of safety; drugs already out there so just seeing if
better; against gold standard; larger pop (is drug equally as effective?)
Phase IV: Post-marketing; optimal use and safety; what is going to happen in population
in general
, 1. changes confirmation (shape) makes possible for receptor to get within nucleus and
bind to DNA (specific sequences) and turn on/off transcription
(1)
Discrete drugs having discrete behaviors because acting on discrete ___________ -
ANSWER-neurons
(1)
Dopamine transporters take neurons from _____________ of cell to ___________ of
cell - ANSWER-outside; inside
** reuptake
** against gradient
(1)
Downregulation vs upregulation - ANSWER-Downregulation = Tolerance
1. AGONIST
2. Excessive transmitter molecules available
3. Chronic stimulation
4. # of receptor sites DECREASES
5. REDUCE effect (desnsitization)
EX: Heroin constantly occupying opiate site then over time the post syn neuron will no
longer respond to normal amounts of heroin (need more)
Upregulation = Sensitization
1. ANTAGONIST
2. don't get any signalling
3. Put more recepotrs out on surface
4. Number of transmitters available at possyn decrease then receptors increase
EX: Antipsychotic meds --> block dopamine receptor --> up reg --> additional receptors
--> overactive -->
If remove the antagonist -- heightened degree of signalling
(1)
Electrical signaling vs chemical signaling - ANSWER-Electrical Signaling --> on/off (hard
to control)
- down axon and to synapse
- within cell
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