(R)-sila-venlafaxine: a selective noradrenaline reuptake inhibitor for the treatment of emesis.
Sila-substitution of drugs (the carbon/silicon switch) is a concept that is being successfully used for the development of new chemical entities. The (R)-sila-analogue of the antidepressant venlafaxine is devoid of the serotonin reuptake inhibition observed with the marketed drug, leading to a selective noradrenaline reuptake inhibitor displaying anti-emetic properties.
Showell
Graham A
GA
Paradigm Therapeutics Ltd, 162 Cambridge Science Park, Milton Road, Cambridge CB4 0GP, UK. gshowell@paradigm-therapeutics.com
Barnes
Matthew J
MJ
Daiss
Jürgen O
JO
Mills
John S
JS
Montana
John G
JG
Tacke
Reinhold
R
Warneck
Julie B H
JB
D000818:Animals; D000932:Antiemetics / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use*; D018360:Crystallography, X-Ray; D003511:Cyclohexanols / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D004195:Disease Models, Animal; D004353:Drug Evaluation, Preclinical; D005289:Ferrets; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D008958:Models, Molecular; D015394:Molecular Structure; D058831:Serotonin 5-HT3 Receptor Antagonists; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D000069470:Venlafaxine Hydrochloride; D014839:Vomiting / Q000188:drug therapy*
D000932:Antiemetics; D003511:Cyclohexanols; D058831:Serotonin 5-HT3 Receptor Antagonists; D017367:Selective Serotonin Reuptake Inhibitors; D000069470:Venlafaxine Hydrochloride