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The eutomer is the enantiomer having the desired pharmacological activity, [4] e.g., as an active ingredient in a drug. The distomer , on the other hand, is the enantiomer of the eutomer which may have undesired bioactivity or may be bio-inert.
An example of such an enantiomer is the sedative thalidomide, which was sold in a number of countries around the world from 1957 until 1961. It was withdrawn from the market when it was found to cause birth defects. One enantiomer caused the desirable sedative effects, while the other, unavoidably [23] present in equal quantities, caused birth ...
An enantiopure drug is a pharmaceutical that is available in one specific enantiomeric form. Most biological molecules (proteins, sugars, etc.) are present in only one of many chiral forms, so different enantiomers of a chiral drug molecule bind differently (or not at all) to target receptors.
The drug was withdrawn from world market when it became evident that the use in pregnancy causes phocomelia (clinical conditions where babies are born with deformed hand and limbs). Later in late 1970s studies indicated that the (R)- enantiomer is an effective sedative, the (S)-enantiomer harbors teratogenic effect and causes fetal abnormalities.
In some cases, the less therapeutically active enantiomer can cause side effects. For example, ( S -naproxen is an analgesic but the ( R -isomer causes renal problems. [ 31 ] In such situations where one of the enantiomers of a racemic drug is active and the other partner has undesirable or toxic effect one may switch from racemate to a single ...
The (R)-enantiomer is -1-aminoindan, which has pharmacological activity and is an active metabolite of the antiparkinsonian agent rasagiline. [2] [4] [5] A number of notable 1-aminoindane derivatives exist. These include the following: 1-Aminoindan-1,5-dicarboxylic acid (AIDA) – selective mGlu 1 receptor antagonist [3] [7]
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Some drug molecules are chiral, and the enantiomers have different effects on biological entities. They can be sold as one enantiomer or as a racemic mixture. Examples include thalidomide, ibuprofen, cetirizine and salbutamol. A well known drug that has different effects depending on its ratio of enantiomers is amphetamine.