Neurotransmitter Receptors & Pharmacology Flashcards
3 sites of cholinergic receptors
- Autonomic ganglionic
- Parasympathetic postganglionic
- Neuromuscular junction
Cholinergic receptor at autonomic ganglionic
Nicotinic N(G)
Parasympathetic postganglionic cholinergic receptor
Muscarinic M(2)
Cholinergic receptor at neuromuscular junction
Nicotinic N(M)
What does belladona target?
Parasympathetic postganglionic muscarinic M(2)
Examples of nicotinic cholinergic ligands
- ACh
- Hexamethonium
- Decamethonium
- Succinylcholine
Hexamethonium is?
Ganlionic antagonist (N(G))→ non-depolarizing blocker
Decamethonium is?
Neuromuscular (N(M)) → depolarizing blocker
How does agonist binding activate receptor?
Induces conformational shift (picture lock and key)
2 major types of metabotropic Nt receptors
- G-protein linked
2. Tyrosine kinase linked
Examples of G-protein linked receptors
- Beta-adrenergic
- M(2) muscarinic
- alpha(1)-adrenergic
- H(1) histaminergic
Receptor associated with G(s)/cAMP pathway
beta-adrenergic
Receptor associated with G(i)/cAMP pathway
M(2) muscarinic
Receptor associated with G(q)/IP(3)/DAG pathway
alpha(1)-adrenergic
Receptor associated with G(q)/NO/cGMP pathway
H(1) histaminergic
2 examples of tyrosine kinase linked receptors
Dopamine and NMDA receptor modulation
How do non-covalent bonds relate to the “lock and key model”?
Agonists will occupy all important non-covalent bond sites to induce change
Beta(2)-adrenergic receptors are found on what organ?
Bronchi
Beta(1)-adrenergic receptors are found on what organ?
Heart
Atenolol
Blocks beta(1) → selective antagonist
