2 - Receptors 101

What is the Greek symbol ε ?

Epsilon

What are some drugs that modifies their targets covalently?

Aspirin / clopidogrel / omeprazole

What is signal transduction (simple terms)?

Passing info on in a different form

What is a superfamily?

Broad grouping of proteins that are related to each other in structure and function

What is adrenoceptors also known as?

Adrenergic receptors

Which 2 adrenoceptors are (the most) important drug targets?

B1 / B2

Where is B1 adrenoceptors heavily expressed? and whats its important role?

The heart / increasing HR and force of contraction

Drugs blocking B1 adrenoceptors would be good for treating which conditions? What is an example of this drug?

Angina / Atenolol

Where are B2 adrenoceptors expressed? and whats its role?

Bronchial smooth muscles / Dilation of the airways

What drug can activate B2 adrenoceptors without having too much effect on B1?

Salbutamol / ventolin

What does pLGICs stand for?

Pentameric ligand gated ion channels

How many subunits do pLGICs have?

5

Which kingdoms of life are pLGICs present in?

All 3

What do all subunits of the pLGICs have?

4 transmembrane domains with a large N terminal extracellular domain

What is nAChRs responsible for? (not in the CNS)

Fast excitatory transmission between motor neurons and skeletal muscles / in autonomic ganglia

What is nAChRs responsible for in the CNS?

Modulate the release of other neurotransmitter

What role of nAChRs makes nicotine addictive?

Ability to modulate the release of the dopamine

What does GABA-A stand for?

y-aminobutyric acid type A

What are GABA-A receptors (when activated)?

Chloride channels

What do activated GABA-A receptors do?

Allow more Cl- to enter the cell, hyperpolarising the cell, making it less excitable

What type of biological molecule is GABA?

Amino acid

What can GABA-A be activated by? (🚩)

Muscimol

What is muscimol?

Main psychoactive compound from fly agaric mushrooms

What % of synapses in the CNS, use GABA as a transmitter?

30

What % of brain neurons produces GABA?

20

What are the 2 classes of GABA receptors?

GABA-A pLGIC / GABA-B

What is GABA-A pLGIC receptors responsible for?

Fast synaptic inhibition

What are GABA-B receptors? and what do they do?

G protein coupled receptors / produce slower inhibition

What is the physiological importance of GABA-A?

Main inhibitory transmitter in the brain

GABA-A receptors are targets for drugs aiming to:_________?

‘damp-down’ activity in the brain

What are some examples of drugs that target GABA-A receptors?

Diazepam / alcohol

How do drugs targeting GABA-A receptors produce their function?

+ve allosteric modulators of the receptor / make receptor work better by binding to allosteric site of GABA-A

What is iGluRs abbreviated for?

ionotropic glutamate receptors

What are the 3 families that iGluRs are divided into?

NMDA receptors / AMPA receptors / kainate receptors

What is NMDA abbreviated for?

N-methyl-D-aspartate