Receptors and drugs Flashcards
Short acting drugs which block AchE?
- Reverisible binding
- Edrophorium
What are A2 adrenergic receptors involved in?
Presynaptic inihibition of noradrenaline release
How many transmembrane domains does an ionotropicc receptor have?
4
What are the unwanted side effects of adrenoreceptor antagonists?
- Bronchoconstriction
- Cardiac depression
- Bradycardia
- Fatigue
How many transmembrane domains does a GPCR have?
7
What drug treats hypertension?
Clonidine (a A2 adrenoreceptor agonist)
Prazoin (A2 adrenoreceptor antagonist)
What type of receptor is mAchR?
GPCR
How is cholinergic transmission enchanced?
By drugs that inhibit acetlycholinasterase
- Present in the CSF, synaptic cleft and cholinergic nerve terminals
Agonist of nAchR?
Nicotine
Antagonist of GABAa?
- Picrotoxin
- Treats seizures
Medium acting drugs which block AchE?
- Slow hydroloysis
- Neostigmine
- Pyridostigmine
Antagonist of nAchR?
Curare
Long acting drugs which block AchE?
- Irreversible binding
- Cross the blood-brain barrier
- Nerve gas
- Pesticides
- Organophosphates
Where are B1 adrenergic receptors present?
In the heart
How many transmembrane domains does a kinase linked receptor have?
1
What type of receptors are adrenergic?
GPCR
Agonist of GABAa?
GABA
Phenobarbitone
Antagonist of opiate receptors?
Naloxone
What does ephedrine treat and how?
Nasal congestion
- B agonist and an indirectly acting sympathomimeitc drug (causing NA release)
B2 adrenoreceptor agonist?
Salbutamol
What is the structure of glutamate receptors?
- 3 Transmembrane domains
- 4 subunits
What does efficacy mean?
The ability of the drug-receptor complex to lead to intracellular signalling
Structure of nAchR?
- 5 subunits, each channel has variations of these 5 subunits but a minimum of 2 alpha subunits are required
- Each subunit has 4 transmembrane domains
- 2 x Ach bind at the interphases between alpha to activate)
Antagonist of mChR?
Atropine