In pharmacological profile

The BioPrint prohle is enriched by 15 years of knowledge and experience in pharmacological profiling. This experience includes an in-depth... 

TABLE 26.4 Differences in pharmacological profile of couples of enantiomers ... 

Comparison between human S-HT- and S-HTjc receptors indicated 50% overall homology, suggesting an evolutionary close relationship [5] as was already suggested from the identical signal-transduction pathways and the close similarity in pharmacological profile [10, 1]. As with the S-HTja receptor, preliminary data have been obtained that the human 5HT2P gene has at least 2 introns. 

The pharmacological profile of buspirone in both animals and humans differs substantially from that of the ben2odia2epine anxiolytics. Buspirone lacks anticonvulsant, myorelaxant, and hypnotic effects. It also produces less sedation resulting in less psychomotor impairment in conjunction with... 

Included in the noimarcotic class of antitussives are many compounds that do not possess a morphine skeleton and which vary widely from each other with respect to stmctural features and pharmacologic profiles. 

Oxolamine [959-14-8] (57) is sold in Europe. It is an oxadiazole, and its general pharmacological profile is described (81). The compound possesses analgesic, antiinflammatory, local anesthetic, and antispasmodic properties, in addition to its antitussive activity. Although a central mechanism may account for some of the activity, peripheral inhibition of the cough reflex may be the dominant effect. The compound has been shown to be clinically effective, although it is less active than codeine (82,83). The synthesis of oxolamine is described (84). 

Ethyl dibunate [5560-69-0] (59), which is sold ia Canada, is the ethyl ester of 3,6-(/ f2 -butyl)-l-naphthalenesulfonic acid. It is stmcturaHy unrelated to most of the classical antitussives and is a selective central inhibitor of the cough reflex. Also significant is its low toxicity. The oral LD q is greater than 5000 mg/kg in the rat. The clinical and pharmacological profile of this compound has been reviewed (89). 

Extension of the alkyl group on the carbon bearing the amine changes the pharmacologic profile. Reductive amination of 1-phenylbutanone-2 (60) with pyrrolidine in formic acid gives pro-litane (61), a central nervous system stimulant agent with antidepressant properties. 

It should be noted that the stereochemistry of the B/C and C/D junctions has remained inviolate in all the modifications discussed to date. It was in fact assumed that changing either of these was a quick path to loss of activity. Just such a modification, however, led to a progestin with a unique pharmacologic profile. 

Nabitan (39) is a cannabis-inspired analgesic whose nitrogen atom was introduced in order to improve water solubility and perhaps to affect the pharmacological profile as well. The phenolic hydroxyl of benzopyran synthon is esterified with 4-(l-piperidino)butyric acid under the influence of dicyclohexyl carbodi mi de. In addition to being hypotensive and... 

Whitebread, S., Hamon, J., Bojanic, D., and Urban, L. (2005). In vitro safety pharmacology profiling An essential tool for successful drug development. Drug Disc. Today 10 1421-1433. 

---