772985
receptor classification -
pharmacodynamics
- Receptor
Superfamilies
- G-Protein Coupled Receptors
- has the most
receptors
using it
- Metabotropic
- several types of
intracellular signal
transduction
- several types of
intracellular signal
transduction
- single
polypeptide
chain
embedded in
the cell
membrane
- traverse
membrane
7 times
- pentamer
- pentamer
- traverse
membrane
7 times
- has the most
receptors
using it
- Ion Channels
- voltage-gated ion
channels
- channels open in response to
changes in voltage across cell
membrane
- Passage of ions:
Na+, K+, Ca2+, Cl-
- Voltage-gated
Na+ channels
- single poly-peptide
chain
- Depolarization
- each domain
becomes activated
- inside of cell has
become more positive as
each domain becomes
activated
- inside of cell has
become more positive as
each domain becomes
activated
- each domain
becomes activated
- BETA SUBUNITS
- regulatory, maintain
appropriate structure
and fxn
- regulatory, maintain
appropriate structure
and fxn
- single poly-peptide
chain
- Voltage-gated
Na+ channels
- Passage of ions:
Na+, K+, Ca2+, Cl-
- 4 domains
V-gated
channel
- 6 segments in
each domain
- change in
voltage
- S4
- S4
- re-entrant loop
- b/t segments 5 and 6
- b/t segments 5 and 6
- segment 6
- local
anesthetics
- bind to
channel
- PREVENT
DEPOLARIZATION
- STOPS PAIN SIGNALS
FROM BEING SENT TO
CNS
- STOPS PAIN SIGNALS
FROM BEING SENT TO
CNS
- PREVENT
DEPOLARIZATION
- bind to
channel
- local
anesthetics
- change in
voltage
- Inactivating
region
- domains 3 and 4
- domains 3 and 4
- 6 segments in
each domain
- lidocaine, novacaine
- cell
response
- prevent
depolarization
- prevent
depolarization
- tissue
response
- block
action
potentials
- block
action
potentials
- organ
response
- loss of
painful
sensation
- loss of
painful
sensation
- cell
response
- channels open in response to
changes in voltage across cell
membrane
- Ligand gated receptors
- aka
ionotropic or
ion channel
receptors
- Endogenous ligands
- ACh, GABA, glutamate,
serotonin, glycine
- agonists
- ACh, GABA, glutamate,
serotonin, glycine
- Na+, Cl+, K+, Ca2-
- Nicotinic
Acetylcholine
Receptor
- Endogenous
ligand Ach
- exogenous ligand:
nicotine
- used by
neuromuscular
blocker drugs
- allosteric modulators bind
to sites other than the
binding site to change
activity of receptor
- Endogenous
ligand Ach
- nerve and muscle
cells, esp.
neuromuscular jxn
- M segments
- traverse membrane
- M1-M4
- M1-M4
- straightens out to
allow flow of Na+
- traverse membrane
- M segments
- quickly
- pentamer
- aka
ionotropic or
ion channel
receptors
- voltage-gated ion
channels
- Enzyme-linked Receptors
- G-Protein Coupled Receptors
- classification based on how cell interacts
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