title: Antagonism of the gerbil's sucrose taste response by p-nitrophenyl alpha-D-glucopyranoside and chloramphenicol.
abstract: We have discovered that the gerbil's chorda tympani nerve response to sucrose is suppressed by p-nitrophenyl alpha-D-glucopyranoside (PNP-Glu) and chloramphenicol (CAP). Mixture experiments of PNP-Glu and CAP with sodium chloride, potassium chloride, hydrochloric acid, and sucrose gave rise to the following observations: Neither PNP-Glu nor CAP alone stimulates the gerbil's taste nerve; while the sucrose response is suppressed by these inhibitors, taste responses produced by sodium chloride, potassium chloride, and hydrochloric acid are unaffected by the presence of PNP-Glu or CAP; the antagonisms of PNP-Glu and CAP were surmounted by a high concentration of sucrose; CAP is a more potent antagonist (IC50 = 0.0013 M) than PNP-Glu (IC50 = 0.022 M), and both are more potent than methyl 4,6-dichloro-4,6-dideoxy-alpha-D-galactopyranoside (IC50 = 0.048 M); and sucrose antagonism occurs only when PNP-Glu and CAP are mixed with sucrose. It is short-lived and ceases when the mixtures are rinsed from the gerbil's tongue. Structure-activity studies provided the following information: The alpha anomer of PNP-Glu is a more potent inhibitor than its beta anomer; among the PNP-Glu derivatives tested (p-aminophenyl, p-nitrophenyl, and phenyl) only p-nitrophenyl inhibited; among the nitrophenyl galactosides, the para derivative was more potent than the ortho or meta; and p-nitrophenyl alpha-D-mannopyranoside and p-nitrophenyl alpha-D-galactoside are slightly more potent than PNP-Glu. On the basis of concentration experiments, we believe that the inhibitory mechanisms of PNP-Glu and CAP are different, which suggests the existence of at least 2 sucrose receptor sites.
mesh_terms: D000818:Animals; D002701:Chloramphenicol / Q000494:pharmacology*; D005849:Gerbillinae; D005960:Glucosides / Q000494:pharmacology*; D006027:Glycosides / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013395:Sucrose / Q000037:antagonists & inhibitors* / Q000502:physiology; D013649:Taste / Q000187:drug effects* / Q000502:physiology
chemical_list: D005960:Glucosides; D006027:Glycosides; C019502:4-nitrophenyl alpha-glucoside; D013395:Sucrose; D002701:Chloramphenicol