Mefloquine belongs to the aryl amino alcohols, a chemical class of antimalarial drugs that includes quinine
The approved drug is a racemic mixture of (R,S)- and (S,R)-enantiomers. We show the chemical structure without stereochemistry to represent the mixture and the non-isomeric structure is also represented in the PubChem and ChEMBL entries listed in the links table below, while the two enantiomers forming the racemate are represented by PubChem CID 40692
and PubChem CID 456309
lists 9 stereoisotopes.
The administerd form contains the mefloquine hydrochloride salt.
tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY.Activity at non-malarial protein targets:
Racemic mefloquine has been identified as an antagonist of the human adenosine A2A
receptors, with nanomolar binding affinities [8
]. The (11R
) isomer of mefloquine (PubChem CID 456309
) has been determined as the most potent A2A
binder, with a Ki
of 61 nM (Ki vs.
receptor is 255 nM) [4
]. It has been suggested that off-target activity at human adenosine receptors may contribute towards the adverse neuropsychiatric side-effects that are associated with mefloquine use.