Drugs 1 - intro

Question 1

full agonist

Answer 1

full effect at less than 100% occupancy (spare receptors)

Question 2

partial agonist

Answer 2

not full effect even at 100% occupancy

Question 3

constitutive receptor activation

Answer 3

receptors are active without a ligand bound

Question 4

drug targets

Answer 4

transporters, enzymes (false substrates), receptors and ion channels (blockers or modulators)

Question 5

drugs on receptors

Answer 5

can wither directly effect ion channel activation or can act transduction mechanisms such as enzyme activation, DNA transcription and ion channel modulation

Question 6

neuroendocrine siganlling

Answer 6

neurohormones are released by neurons in the brain where they diffuse inTo the CSF and blood stream where they can travel to the rest of the brain and body

Question 7

synaptic transmission

Answer 7

transmitters released into a small space between cells where they diffuse to a receptor dense area on the post synaptic cell

Question 8

Autocrine

Answer 8

paracrine release but acts on itself to inhibit or activate the cell

Question 9

types of signalling molecules

Answer 9

amino acids, catecholamines, lipids/streroids, small molecules, peptides

Question 10

amino acids 
time:
target:
action:
transmission:

Answer 10

GABA and glutamate act in the order of ms on ligand gated ion channels and GPCRs to inhibit or excite cells. - fast transmission

Question 11

Catecholamines 
time:
target:
action:
transmission:

Answer 11

Include noradrenaline, dopamine and adrenaline and ACh
They act in the order of seconds on GPCRs (and ms in nAChRs) to modulate or excite inhibit. they can act via fast or slow transmission

Question 12

Peptides

Answer 12

neuropeptide y, substance p
seconds to minutes
act on GPCRs and second messengers to modulate

Question 13

synaptic plasticity takes…

Answer 13

days and is carried out by sLow transmitters such (catecholamines) and NO

Question 14

which drug targets take hours?

Answer 14

nuclear and kinase linked receptors (as they both work via protein synthesis)

Question 15

Specialisations of the brain

Answer 15

CFS, BBB, Blood supply (18% O2, 2% body mass), lack of regeneration (glial cells)

Question 16

CSF journey

Answer 16

4th ventricle, subarachnoid space, back to brain via the subarachnoid cisterns, bathes tissues, filtered back through the arachnoid villi. Replaced every 6-7 hours

Question 17

Specialisation of CSF

Answer 17

physical and chemical isolation - plasma transudate - body capillaies = fenestrated. brain capillaries = tight junctions, pericyte cells, basement membrane, astroglial processes.

Question 18

meningitis

Answer 18

usually injection of drugs causes a rise in plasma levels and then slowly decline - not mirrored in the CSF - it is in inflammatory disorders of the BBB as it becomes more leaky