10.0 Drug List Flashcards
(203 cards)
Vesamicol
Non-competative and reversible blocker of VAChT
Varenicline
High affinity partial agonist for the α4β2nAChRs<div>High affinity full agonst for the α7nAChRs</div>
Trimetaphan
Competative antagonist of the (α3)2(β2)3isoform of the nAChR
Hexamethonium
Competative antagonist of the (α3)2(β2)3isoform of the nAChR
Tetramethylammonium (TMA)
Neuronal (Nn) nAChR agonist
Dimethylphenylpiperazinium (DMPP)
Neuronal (Nn) nAChR agonist
Suxamethonium
Depolarising nAChR antagonist that initially activates the receptor but isnt hydrolysed by AChE so causes a secondary antagonism
Curare (d-tubocurarine)
Non-depolarising nAChR antagonist
Pancuronium
Synthetic non-depolarising aminosteriod nAChR antagonist
Rocuronium
Synthetic non-depolarising aminosteriod nAChR antagonist
Atracurium
Synthetic non-depolarising nAChR antagonist (benzylisoquinolinium)
Mivacurium
Synthetic non-depolarising nAChR antagonist (benzylisoquinolinium)
Botulinum toxin (BTx)
Peptidase that cleaves SNARE proteins to prevent release of ACh, hence blocking cholinergic neurotransmission
α-bungarotoxin
Irreversibly binds to the ACh binding site on the adult nAChR hence blocking cholinergic neurotransmission
β-bungarotoxin
Inhibits ACh release through a mechanism thought to involve phospholipase A2, which leads to blockage of cholinergic neurotransmission
α-lacrotoxin
Causes massive release and subsequent depletion of ACh at the NMJ thought to be due to its ability to form a Ca2+channel
Tetanus neurotoxin
Cleaves synaptobrevin to prevent glycine release by inhibitory interneurones upsteam of those innervating skeletal muscle
Bethanechol
Choline ester that acts as a non-selective agonist of mAChRs
Pilocarpine
mAChR agonist that is stable to hydrolysis by AChE
Atropine
Non-selective mAChR antagonist
Scopoloamine
Non-selective mAChR antagonist
Homatropine
Non-selective mAChR antagonist
Methscopolamine
Non-selective mAChR antagonist
Ipratropium
Short-acting non-selective mAChR antagonist (SAMA) with some selectivity for M3receptors in the airways
- Acts on β3 (or β2) subunit of the GABAA receptor resulting in Cl- influx and hyperpolarisation of the postsynaptic membrane