Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

LAST MEDCHEM OF UR LIFE > 37 - Transporters > Flashcards

37 - Transporters Flashcards

1
Q

Diazepam

Target WHAT? // Indication

A

Ligand-Gated GABA Channels

SEDATIVE

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Target of SSRI’s
Fluoxetine / Sertraline / Citalopram
MoA

A
  • *SERT**
  • *Serotonin Transporter**

is involved in serotonin being
REUPTAKEN** –> back into the **PRE-synaptic neuron
INHIBITION
leads to MORE Serotonin in the Synaptic Cleft
VVVVV
Improve depression symptoms

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What type of Transporter PROTEIN?

Water-filled –> extend across the cell membrane

GATED = closed or open

Involve Charged solutes
required to be transported rapidly across the membrane

A

CHANNELS

Ion Channels

Ex. of GATED channels:
Voltage-Gated Channels
open in response to magnitude of membrane potentials

Ligand-Gated channels
open in the presence of a specific ligand

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

How can ion channels discriminate between ions?

A

SELECTIVITY FILTER
these sites allow for the transporter protein to
FEEL IONS by
DEHYDRATION which Cost energy
but, Since the channels contain Oxygen-lined binding sites
these OFFSET the energy of Dehydration

important in distinguishing
Na+ vs K is the SIZE of the CAVITY

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

How are ION CHANNELS

CLASSIFIED?

A

Based on:
WHAT
leads to the Channel Opening/Closing
&
the TYPE of ION that is transported

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

A collection of protein domains that together create a water‐filled pore to allow the passage of ions through a cell membrane in response to: chemical stimuli, temperature changes, or mechanical forces

What is this?

A

ION CHANNEL

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Excitable Cells & ION CHANNELS

A

Neurons / Muscle cells / Touch Receptors
are all excitable cells that use Ion channels to convert chemical/mechanical messages into:
ELECTRICAL SIGNALS

allow for RAPID ION MOVEMENT –> electrical signal

Self-propagting Electrical Signal
that can travel down the entire length of a cell

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

SERT = Serotonin Transporter

Facts:

A

ACTIVE TRANSPORTER = CARRIER
Belongs to the
NSS = NT Sodium SYMPORTER family
which also includes
Dopamine + NorEpinephrine Transporters

  • *Na &** Serotinin
  • -> REEnters the Pre-synpaptic cell
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Physiological Necessity of
ION CHANNELS

A

generate ELECTRICAL SIGNALS

used to regulate CELL VOLUME

GRADIENTS
can be built across membranes using ion pumps
(lysosomes)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What type of TRANSPORT?

Thermodynamically favorable

Solutes transported from:
HIGH –> low conentrations

no ENERGY (ATP) required

A

PASSIVE TRANSPORT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

DRUGS that target VOLTAGE-Gated Ion Channels

A

VOLTAGE GATED

  • *Verapamil**
  • *calcium** channels –> CCB –> HT
  • *Lidocaine**
  • *sodium** channel –> local anesthetic
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Biosynthesis of Serotonin (5-HT)

A

Tryptophan = Trp
VVVV
Trp Hydroxylase + O2
VVVV
5-hydroxy-tryptophan — Decarboxylase
VVVV
5-HT = Serotonin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Example of DRUG that targets:
Neurotransmitter Carriers
transporters

A

SSRIs
Fluoxetine / Sertraline / Citalopram
Prozac / Zoloft / Celexa

INDICATION:

  • *Depression / Anorexia / Bulimia**
  • *OCD** / Panic+Anxiety Disorder
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

SSRI’s ONSET

A

Continue therapy for 4-6 weeks
SSRI’s have a slow onset

take for at least 8 weeks

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Role of SEROTONIN:

5-HT

A
  • *Serotonergic Signaling** influences
  • *Neurologic processes** such as

Sleep / MOOD / cognition

Pain / hunger / aggression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Verapamil

Targets WHAT // Indicated for?

A

VOLTAGE GATED CALCIUM CHANNELS

CCB for HT

17
Q

What MOLECULES are required in SERT?

A
  • *SODIUM_ + _CHLORIDE** + K
  • *Sodium Symporter**

conformational change

Na+ INFLUX along it’s concentration gradient
= driving force

18
Q
  • *Ion Channels**
  • *Critical Roles in:**
A

Nerve / Muscle relaxation

COGNITION / Sensory Transduction

regulation of BLOOD PRESSURE

Cell Proliferation

19
Q

Transporter Proteins
& why ther are needed

Drug targets:
Receptors > Enzymes > Transporters 15%
most common therapeutic action:
Anti-Hypertensive // Anti-arrhythmia

A

Facilitate the movement of specific substances:
Ions / Nutrients / Metabolites
across CELL MEMBRANES

Mediate:
Facilitated / Passive Transport
&
ACTIVE Transport

20
Q

How do SSRI’s bind to SERT?

KNOW THIS ONE

A

SSRI’S BIND TWO SITES ON SERT

ALLOSTERIC SITE
which obstructs the release of drug bound to central site
LOCKS –> prevents/slows SSRI from leaving

Central Binding Site
block SERT in a configuration OPEN to the OUTSIDE to the neuron
prevents serotonin binding & further motion

21
Q

Drug that targets Ligand-Gated Ion Channels

A

Varenicline = Chantix
acetylcholine‐gated ion channels
Partial Agonist for SMOKING CESSATION

  • *Diazepam**
  • *Gaba** channels –> sedative
22
Q

Lidocaine & Bupivacaine

Target WHAT? // Indication

A

Voltage-Gated Sodium Channels

LOCAL ANESTHETIC

23
Q

MECHANISM of SERT

A

SYMPORTER
which is driven by the Na+ influx along it’s concentration gradient
(Na is HIGH OUTSIDE –> wants to ENTER the cell)

  • Open to outside of cell:
    • Na & Serotonin & Cl
  • Conformational change
  • Opens INSIDE of cell
    • Na + Serotonin enter the cell
  • K+ & Cl in the symporter
    • K+ OUT
24
Q

How does Varenicline help smoking cessation?
Chantix

A

Partial Agonist
of a AcetylCholine-Gated Ion Channel
VVVVV
Elicits a Moderate / Sustained INCREASE in DOPAMINE LEVELS
which causes a Reduction in craving
VVVVVV
SHIELDING the smoke from producing a
nicotine-induced DOPAMENIRGIC activation
NO REWARD SYSTEM FROM SMOKING

25
Q

Varenicline

Target WHAT? // Indication

A

Partial Agonist
of LIGAND GATED ION CHANNEL

Smoking Cessation

CHANTIX

26
Q

What type of ​TRANSPORT?

Thermodynamically UN-favorable

Solutes transported from:
low –> HIGH concentrations

requires ENERGY ATP

A

ACTIVE TRANSPORT

Proton pump

27
Q

ION CHANNEL
FUNCTION

A

Gated & Water Filled PORES
that permit the FLUX of IONS down their
EC Potential Gradient = PASSIVE

Na / K / Cl / Ca

Na/Ca OUT

K IN

28
Q

What type of Transporter PROTEIN?​

undergo CONFORMATIONAL change
which dilivers solute to other side

SELECTIVITY of their solutes
that are permitted to enter or exit

A

CARRIER
Transporter Protein

Neurotransmitter Carrier

LAST MEDCHEM OF UR LIFE (11 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions