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Anorexiant activity of individual phenylpropanolamine (PPA) enantiomers
ABSTRACTS
224 Anorexiant Enantiomers.
Activity
of
Individual
Phenylpropano,lamine
(PPA)
TIMOTHY J. MAHER and MARC S. EISENBERG. Departmenf Pharmacology, Massachusetts College of Pharmacy, Boston, MA 02115, U.S.A.
of
Racemic PPA (d,l-norephedrine; d&NOR) decreases food intake in both laboratory animals and humans. Experiments were performed in rats to determine the contribution of each enantioner to PPA’s anorexiant activity. Food intake was stimulated by 24 h food deprivation (FD), 8OOmg/kg 2-deoxyglucose (2-DG) and lOOU/kg insulin (INS) and measured 1 and 3 h later. d-NOR (75-150mg/kg) dose-dependently reduced food intake stimulated by FD (69.95x, 34--78x), 2-DG (72-96x, 79-94x) and INS (&t-96%, 52-86x) at 1 and 3 h, respectively. l-NOR (7.515mg/kg) also reduced food intake, FD (3448x, 26--33x), 2-DG (&l--90%, 2743%) and INS (83-95%, 2849%). These results demonstrate Z-NOR to be approximately seven times more potent than d-NOR. Insulin Binding Normoglycemic
and Glucose Utilization in Brain of Hyperinsulinemic Bats. P. MARFAING, L. PENICAUD, Y, BROER and L. PICON.
Laboratory of Physiological Development UA 307 CNRS, Universitb Paris Vii, Paris, France and INSERM, U.55, H6pital St Antoine, 75571 Paris Cedex 12, France.
The aim of the present work was to study the effects of insulin, using the euglycemic hyperinsulinemic clamp, on insulin binding and glucose utilization in specific brain areas by autoradiographic methods. Conscious and unrestrained female rats were submitted to a 90min infusion of insulin (06 U/kg/h) while glycemia was maintained at the basal value (88 mg/dl). Compared to controls the density of insulin binding was significantly higher (p
U.S.A.
The microdialysis technique was used to determine the extent to which dopamine (DA) output in the NAC could be manipulated by salt or water intake or development of a CTA to saccharin. Extracellular DA increased during water intake in response to deprivation or i.c.v. angiotensin. Similarly, DA release increased during salt intake in response to sodium depletion and a small increase occurred when subjects tasted saccharin for the first time. Conversely, after taste aversion conditioning, saccharin infused into the mouth caused a decrease in accumbens DA. These results suggest that the positive and negative hedonic quality of a stimulus may be translated into increased and decreased mesolimbic dopamine output. Anti-natriorexic
Action
M. PERFUMI and G. Camerino, Italy.
DE
of Tachykinins. M. MASSI, C. POLIDORI, L. GENTILI, CARO. Institute of Pharmacology, University of Camerino, 62032
The anti-natriorexic effect of tachykinins (TKs) was investigated on salt intake induced by: (1) sodium depletion, (2) subcutaneous DOCA treatment, (3) intracerebroventricular (i.c.v.) renin injection, as well as (4) on the “need-free” salt intake of multidepleted female rats. TKs endowed with high activity at NK-3 receptors were the most potent antinatriorexic agents. Following i.c.v. injection TKs showed a wide spectrum of action, by inhibiting salt intake in all the experimental models. When given into the medial amygdala their action was selective for the angiotensinergic
224 Anorexiant Enantiomers.
Activity
of
Individual
Phenylpropano,lamine
(PPA)
TIMOTHY J. MAHER and MARC S. EISENBERG. Departmenf Pharmacology, Massachusetts College of Pharmacy, Boston, MA 02115, U.S.A.
of
Racemic PPA (d,l-norephedrine; d&NOR) decreases food intake in both laboratory animals and humans. Experiments were performed in rats to determine the contribution of each enantioner to PPA’s anorexiant activity. Food intake was stimulated by 24 h food deprivation (FD), 8OOmg/kg 2-deoxyglucose (2-DG) and lOOU/kg insulin (INS) and measured 1 and 3 h later. d-NOR (75-150mg/kg) dose-dependently reduced food intake stimulated by FD (69.95x, 34--78x), 2-DG (72-96x, 79-94x) and INS (&t-96%, 52-86x) at 1 and 3 h, respectively. l-NOR (7.515mg/kg) also reduced food intake, FD (3448x, 26--33x), 2-DG (&l--90%, 2743%) and INS (83-95%, 2849%). These results demonstrate Z-NOR to be approximately seven times more potent than d-NOR. Insulin Binding Normoglycemic
and Glucose Utilization in Brain of Hyperinsulinemic Bats. P. MARFAING, L. PENICAUD, Y, BROER and L. PICON.
Laboratory of Physiological Development UA 307 CNRS, Universitb Paris Vii, Paris, France and INSERM, U.55, H6pital St Antoine, 75571 Paris Cedex 12, France.
The aim of the present work was to study the effects of insulin, using the euglycemic hyperinsulinemic clamp, on insulin binding and glucose utilization in specific brain areas by autoradiographic methods. Conscious and unrestrained female rats were submitted to a 90min infusion of insulin (06 U/kg/h) while glycemia was maintained at the basal value (88 mg/dl). Compared to controls the density of insulin binding was significantly higher (p
U.S.A.
The microdialysis technique was used to determine the extent to which dopamine (DA) output in the NAC could be manipulated by salt or water intake or development of a CTA to saccharin. Extracellular DA increased during water intake in response to deprivation or i.c.v. angiotensin. Similarly, DA release increased during salt intake in response to sodium depletion and a small increase occurred when subjects tasted saccharin for the first time. Conversely, after taste aversion conditioning, saccharin infused into the mouth caused a decrease in accumbens DA. These results suggest that the positive and negative hedonic quality of a stimulus may be translated into increased and decreased mesolimbic dopamine output. Anti-natriorexic
Action
M. PERFUMI and G. Camerino, Italy.
DE
of Tachykinins. M. MASSI, C. POLIDORI, L. GENTILI, CARO. Institute of Pharmacology, University of Camerino, 62032
The anti-natriorexic effect of tachykinins (TKs) was investigated on salt intake induced by: (1) sodium depletion, (2) subcutaneous DOCA treatment, (3) intracerebroventricular (i.c.v.) renin injection, as well as (4) on the “need-free” salt intake of multidepleted female rats. TKs endowed with high activity at NK-3 receptors were the most potent antinatriorexic agents. Following i.c.v. injection TKs showed a wide spectrum of action, by inhibiting salt intake in all the experimental models. When given into the medial amygdala their action was selective for the angiotensinergic