Anti-tussive activity

The salt of citric acid and 3-phenyl-5-diethylaminoethyl oxadiazole which possesses an anti-tussive activity, is known under the trade names "Oxolamine", "Perebron and "Bredon 22a). 

Compound N—O N=C—R Antispasmodic activity in vitro) Local anaesthetic activity Analgesic and anti-inflammatory activity Anti-inflammatory activity Central anti-tussive activity ( ) Antitussive activity b)... 

Compounds (27) and (28) have shown dopaminergic activity in rats, but to a lower extent than ( - )-apomorphine. Glaucine shows definite anti-tussive activity," and its tetrahydroxy-derivative exhibits anti-thrombic action. ... 

Mitragynine. Mitragynine (62) ethanedisulfonate exhibits analgesic and anti-tussive properties in animals (335). It has only weak respiratory depressant activity. 

There are also known cases of drug enantiomers that possess completely different therapeutic properties. The (+)-2/ ,35 -stereoisomer of propoxyphene (dextropropoxyphene) is marketed as an analgesic agent, whereas its enantiomer ( )-(25, 3/ )-propoxyphene (levopropoxyphene) is available as an effective anti-tussive agent [3]. The enantiomers of some chiral drugs are known to possess essentially identical qualitative and quantitative pharmacological activities, for example, the antihistamine promethazine, which is marketed as a racemate [5]. 

New applications of dioxolanes include the use of 37 as an anti-tussive , use of the dioxolane-containing furocoumarin dimer paradisin C 38, a natural product isolated from grapefruit, as a cytochrome P450 enzyme inhibitor <02T6631> and use of dioxolane 39 to activate wheat seeds towards germination and protect plants from water... 

Semi-Synthetic Transformations of the Morphine Alkaloids Although it has been synthesised (ref 61), (now by four distinct routes) morphine (63), a powerful analgesic is readily available from the natural source, opium obtained from Papaver somniferum as the major alkaloid present (approx. 10%) and indeed the first to be isolated by Serturner in 1803, while the methyl ether, codeine (64) which comprises only 0.5% is relatively weakly active. Thebaine (65) a third component of opium is non-analgesic but is important as an intermediate for the formation of codeine, a somewhat scarce commodity (ref. 62) but a valuable mild analgesic and anti-tussive in great demand. It is best prepared from morphine by methylation with phenyl trimethylammonium ethoxide the by-product consisting of dimethylaniline (ref.63). 

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