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Pharm > Receptors & Channels > Flashcards

Receptors & Channels Flashcards

1
Q

Receptor

A

Single or group of proteins that allow cell to collect info about surroundings

Dynamic: moving b/w active / inactive

normal points of control in physiologic processes

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2
Q

Ligand

A

chemical messenger that binds and stabilizes a conformation of receptor
(small mlc / peptide)

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3
Q

Conformation Change

A

receptor shape change ->
downstream signal transduction

Most receptors fluctuate b/w:
active /partially active /inactive

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4
Q

Drugs hijack body system

A

Drugs mimic or block body’s own regulatory mlcs

don’t give cell new fx

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5
Q

Ligand combine w/ receptor ….

Agonist
vs
Antagonist

A

to stimulate target organ (activate)
-stabilize active conformation

to interferes w/ naturally occurring agonist or agonist drug (prevent from activating)

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6
Q

Potency vs efficacy

A

Potency = affinity for receptor
Efficacy = intrinsic activity
how much response

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7
Q

Orthosteric antagonist

A

act on main binding site of receptor

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8
Q

Allosteric antagonist

A

act on accessory binding site of receptor

Ex: Benzo (work on GABA but not at site)

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9
Q

Pore Blocker

A

physically obstruct channel

Ex: local anesthetic

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10
Q

Partial Agonist

A

weakly stabilize active state
OR
stabilize partially active state

-> antagonist if fill up all receptors

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11
Q

Inverse Agonist

A

stabilize inactive state (shutdown)
-reverse baseline receptor activity

Ex: B blocker

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12
Q

Non-Competitive Antagonist

A

< max response achievable w/ agonist

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13
Q

Competitive Antagonist

A

Max response of agonist not reduced

Increase the amount of agonist required to produce same intensity of reponse

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14
Q

Ligand Gated Ion Channels

Basics

A

In membrane
Direct coupling
Ex: Nicotinic, ACh, GABAa
oligomeric assembly of subunits around central pore

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15
Q

G Protein-coupled receptors

Basics

A

In membrane [channel or enzyme effector]
Coupled w/ G protein or arrestin
Ex: muscarinic ACh, adrenorecptor

Monomeric/ oligomeric assembly of subunits
w/ 7 transmembrane helicies
w/ intracellular G protein coupling domain

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16
Q

Receptor Kinases

Basics

A

In membrane
protein kinase effector
direct coupling
Ex: insulin, growth factor, cytokine receptor

Single transmembrane helix ->
links extracellular domain to intracellular kinase domain

17
Q

Nuclear receptors

basics

A

Located intracellular
Gene transcription = effector
Coupling via DNA
Ex: steroid receptors

Monomeric structure w/ receptor and DNA binding domains

18
Q

Excitatory
vs
Inhibitory

A

inside of cell charge -> 0
generally letting + ions into cell
[Depolarization]

Inside of cell charge -> more -
generally let -ions into cell (Cl-)
[Hyperpolarization]

19
Q

Ligand Gated Ion Channel
Speed
Families

A

Fast transmission
agonist binding = open pore

Cys Loop receptor
Ionotropic Glutamate Receptor

20
Q

Cys Loop receptor Family

A

Excitatory: Nicotinic ACh, 5HT-3
Inhibitory: Glycine, GABAa
Pentamer: 5 subunits
Named for disulfide bond b/w cisternes near N terminus

21
Q

Drugs that act on Cys Loop Receptors

A

Nic ACh: nicotine, varenicline (chantix)

GABAa: ambien (zolpidem), barbiturates, benzos, alcohol

22
Q

Dugs that act on Glutamate Receptors

A

NMDA: ketamine
AMPA: aniracetam

23
Q

nACh subunits

A

in NMJ contain:
apha beta gama delta subunits

Neuronal nACh:
alpha and beta subunits

24
Q

Chronic nicotine + nACh Receptors

A

(ie smoking) = upregulation

25
Q

nACh receptor activation States

A

Closed
Open (ligand on)
Desensitized (ligand on but not open)
^inactivated closed state

26
Q

Inotropic Glutamate Recptors

A 
AMPA, NMDA, Kainate
Tetramer: 4 subunits
   each has 4 transmembrane domains
       2nd TM domain -> pore
   all 4 binded to open
Excitatory pass Na/K+
27
Q

NMDA receptor

A

can pass Na/K/Ca+ ions
2 subunits bind for glutamate
2 subunits bind for glycine
blocked by Mg+ @ RMP

28
Q

Long Term Potentiation

A

More often neuron fires, stronger synapse gets

Ex: learning/ memory

29
Q

NMDA Receptor

-> coincidence receptor

A

NMDA pass Ca++ ->
activate Ca Calmodulin Kinase 2 [CaMKII]
-> AMPA receptors added to synapse

> AMPA receptors =stronger synapse

Pharm (10 decks)

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