50. Receptors and Signalling Flashcards by Poppy Lamb

what type of receptor is bound and activated by the neurotransmitters/hormones - adrenaline and noradrenaline

G protein coupled adrenoreceptors

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alpha 1 is Ga….
activation of phosp….. …
Increase of I…. and D…
contraction of ?

Gaq
Phospholipid C
IP3 and DAG
vascular smooth muscle

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alpha 2 Ga…
inhibition of ……
decrease of c…..
increase of ….. channels
decrease of …… channels
relaxation of the….
Inhibition of n……

Gai
adenylyl cyclase
cAMP
K+ channels
GI tract
noradrenaline

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Beta 1 is Ga…
stimulation of aden…..
increase of c….
Increased

Gas
adenylyl cyclase
cAMP
Heart rate and cardiac muscle contraction

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Beta 2 is Ga…
stimulation of aden…..
increase of c….
Dilation of the

Gas
adenylyl cyclase
cAMP
Bronchi
(also incr. HR but to a lesser extent than B1)

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Beta 3 is Ga…
stimulation of aden…..
increase of c….
causes……

Gas
adenylyl cyclase
cAMP
Thermogenesis in skeletal muscle

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what binds/activates B2 adrenoreceptors to cause bronchodilation for asthmatic patients

salbutamol

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what binds/activates B1 and B2 adrenoreceptors to cause bronchodilation and has a massive side effect of Tachycardia

Isoprenaline

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name some of Beta1 agonists

Noradrenaline
Adrenaline
Pindolol (partial )

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name some of Beta2 agonists

Adrenaline
Noradrenaline
Salbutamol
Salmeterol
Pindolol (partial)

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name 6 beta blockers (antagonists)

Bisoprolol
atenolol
propranol
metoprolol
carvedilol
sotalol

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Receptors may be divided into 4 main ‘super-families’ or classes based upon their common structure and function?
name them.

Ligand gated ion channels
G protein coupled receptors
Kinase linked receptors
nuclear receptors

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Give an example of a Ligand gated ion channel

Nicotinic acetylcholine receptor

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Nicotinic acetylcholine receptor are permeable to what?

Na+, K+ and Ca2+

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what do Nicotinic acetylcholine receptors do

Modulate fast synaptic excitation in the nervous system - excitatory post-synaptic potentials (EPSPs) and motor endplate potentials (EPPs). Also expressed on the post-ganglionic neuronal cell bodies in the autonomic nervous system

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Drugs that act at as agonists at nicotinic acetylcholine receptors (nAChRs) are…?

acetylcholine
Nicotine
Varenicline (partial)

which drug is a phosphodiesterase inhibitor -> inndicated fro COPD

Theophylline

kinase linked receptors are

insulin receptors

kinase linked receptors are also called

enzyme coupled receptors

kinase linked receptors, when activated cause

parallel signaling cascades

Nuclear receptors are generally bound by….

steroid hormones

Nuclear receptors are ……….so are not …………. to the cell membrane

Intracellular…. Bound.

Nuclear receptors contain

DNA binding domains allowing for the control for gene transcription

what is the nuclear receptor structure

N-AF1-DBD-Hinge-LBD-AF2-C

AF-activation function site
DBD- DNA binding domain
LBD-Ligand binding domain

steroid hormones are ......... and pass through the plasma membrane to bind to nuclear receptors

Lipophillic

Drug Targets can be divided into 4 main categories:

1. Receptors 2. Enzymes 3. Ion Channels 4. Carrier Proteins

what is ibuprofen

a non steroidal anti inflammatory drug (NSAID) that acts at cyclooxygenase enzymes

how does ibuprofen work

It works by blocking enzymes in your body known as cyclooxygenase enzymes (COX-1 and COX-2). These enzymes usually help produce substances called prostaglandins. Prostaglandins are involved in causing pain, swelling, and inflammation by making blood vessels widen (vasodilation).

what side effects for taking ibuprofen

Irritation of the GI tract, possible impairment of renal function via inhibition of prostaglandin-evoked vasodilation.

what kind of drug is amlodipine

calcium channel blocker (antihypertensive)

when is amlodipine used

when a patient has angina and/or hypertension

how does amlodipine work

Calcium channel blocker so is an antagonist at Cav1.3 however slow association and long duration of action

what are SSRIs and what are they commonly used to treat

SSRIs stand for Selective Serotonin Reuptake Inhibitors. They are a class of drugs commonly used to treat depression and anxiety disorders.

what is SERT

Serotonin Transporter. It's a protein that plays a crucial role in the brain's serotonin system.

what is the function of SERT

is responsible for transporting serotonin, a neurotransmitter, from the space between nerve cells (the synaptic cleft) back into the nerve cell that released it (the presynaptic neuron). This process is known as serotonin reuptake.

so what is the role in SSRIs in reducing depression

SSRIs (Selective Serotonin Reuptake Inhibitors) work by blocking SERT. This inhibition increases the amount of serotonin available in the synaptic cleft, which can help improve mood and reduce anxiety

name some drugs that act as SSRIs (antagonists at SERT)

Citalopram Escitalopram Fluoxetine Fluvoxamine Paroxetine Sertraline

Sodium Valproate is used to treat who?

Epileptic people

Sodium Valproate has many what....

mechanisms of action