Development of high-affinity 5-HT3 receptor antagonists. 1. Initial structure-activity relationship of novel benzamides was written by Youssefyeh, R. D.;Campbell, H. F.;Klein, S.;Airey, J. E.;Darkes, P.;Powers, M.;Schnapper, M.;Neuenschwander, K.;Fitzpatrick, L. R.. And the article was included in Journal of Medicinal Chemistry in 1992.Recommanded Product: 3438-16-2 This article mentions the following:
Novel benzamides, e.g. I (X = H, Cl, Br, n = 1; X = Cl, n = 2), II (R = Me, Me2CHCH2, CH2:CHCHMe, MeCOCHMe), and S–III which are orally active, highly potent, specific antagonists of serotonin 5-HT3 receptors were prepared and the structure-activity relationships that led to these novel structures with improved potency in selectivity are described. (S)-III was identified and selected for further evaluation as a 5-HT3 receptor antagonist. Compared with 5-HT3 antagonists such as GR 38032F, BRL 43694, and metoclopramide, (S)-III was most active in (a) inhibiting binding to 5-HT3 receptor binding sites in rat entorhinal cortex with a Ki value of 0.19 nM and (b) blocking cisplatin-induced emesis in the ferret with an ED50 value determined to be 9 mg/kg, i.d. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2Recommanded Product: 3438-16-2).
5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Recommanded Product: 3438-16-2
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics