Advances in Experimental Medicine and Biology, 1993
1. Adv Exp Med Biol. 1993;335:21-8. Consequences of opiate-dependency in a monkey model of AIDS. ... more 1. Adv Exp Med Biol. 1993;335:21-8. Consequences of opiate-dependency in a monkey model of AIDS. Donahoe RM, Byrd LD, McClure HM, Fultz P, Brantley M, Marsteller F, Ansari AA, Wenzel D, Aceto M. Dept. of Psychiatry, Emory Univ., Atlanta, GA 30306. ...
Buspirone (CAS 36505-84-7) was evaluated in three animal models which were designed to study stag... more Buspirone (CAS 36505-84-7) was evaluated in three animal models which were designed to study stages of drug abuse most likely associated with compulsive abuse. Buspirone attenuated abrupt withdrawal in rhesus monkeys maximally-dependent on morphine. In addition, it completely blocked the emergence of cocaine-induced stereotyped behavior in rats and attenuated the hyperarousal or rausch syndrome in morphine-dependent and non-dependent rhesus monkeys. Buspirone was active at doses which caused little, if any, impairment in the animals. The results suggest that buspirone may possibly find application in the pharmacotherapy of opioid and cocaine abuse.
ABSTRACT Cocaine and pipradrol facilitated the avoidance performance of rats in Skinner boxes. Wh... more ABSTRACT Cocaine and pipradrol facilitated the avoidance performance of rats in Skinner boxes. When the drugs were withdrawn performance deteriorated to levels shown by rats that had never been drugged. The drugs seemed to temporarily affect either emotionality or activity rather than to permanently affect learning. Tricyanoaminopropene did not affect performance.
Nicotine produced antinociception in mice which was antagonized noncompetitively by naloxone. In ... more Nicotine produced antinociception in mice which was antagonized noncompetitively by naloxone. In addition, at significantly lower doses, nicotine noncompetitively antagonized morphine-induced antinociception. A speculative suggestion regarding the opiatergic and anti-opiatergic actions of nicotine is that it significantly promotes and maintains smoking behavior.
Journal of comparative and physiological psychology, 1968
... JACK PEARL, MARIO D. ACETO, AND JOHN J. FITZGERALD Sterling-Winthrop Research Institute, Rens... more ... JACK PEARL, MARIO D. ACETO, AND JOHN J. FITZGERALD Sterling-Winthrop Research Institute, Rensselaer, New York Pipradol and cocaine ... stimulants improve the avoidance performance of rats when in-jections are given before testing: ampheta-mines (Hearst & Whalen ...
Writhing was produced in mice by injecting them intraperitoneally with phenylquinone either 10 or... more Writhing was produced in mice by injecting them intraperitoneally with phenylquinone either 10 or 20 min before the start of scoring. The activity of two antiwrithing agents was compared: morphine and nalorphine at doses of 0.5 and 2.0 mg/kg injected subcutaneously 10, 20, or 40 min before scoring. Analyses of both quantal and graded data indicated that the antiwrithing activity
Mice were given a drug per os and 2 h later were challenged with an intravenous LD95 of nicotine.... more Mice were given a drug per os and 2 h later were challenged with an intravenous LD95 of nicotine. Amitriptyline, imipramine, doxepin, meprobamate, chlordiazepoxide, diazepam, trifluoroperazine, haloperidol, thioridazine, chlorpromazine, phenobarbital, propranolol and diphenylhydantoin were all active in protecting mice from extensor convulsions and lethality. Iproniazid, tranylcypromine, atropine, benztropine and trimethadione were inactive. There appears to be a relationship between blockage of nicotine-induced extensor convulsions and lethality in mice and sedative-antianxiety effects in man. This relationship is especially good for drugs designated antidepressant, antianxiety and antipsychotic.
Each of the dynorphin A(1-13) or dynorphin (dyn) treatment groups receiving naloxone showed a sig... more Each of the dynorphin A(1-13) or dynorphin (dyn) treatment groups receiving naloxone showed a significant overall reduction of overt signs compared with the dyn controls. The data suggested that the overt psychomotor effects of dyn in the rhesus monkey were especially prone to blockade by naloxone, and probably involved opioid mechanisms.
The resolution of racemic nicotine to provide optically pure (+)-nicotine and the synthesis of ra... more The resolution of racemic nicotine to provide optically pure (+)-nicotine and the synthesis of radiolabeled nicotine with high specific activity have facilitated the study of nicotine binding in brain. The actions of the stereoisomers of nicotine on the central nervous system are qualitatively similar in most tests but (-)-nicotine is more potent than the unnatural (+)-isomer by 10-fold or greater. Binding of radiolabeled nicotine to brain has both saturable and nonsaturable components. Only saturable binding is affected by incubation conditions such as time, temperature, pH and ion concentration. Excess concentrations of the stereoisomers are equally effective in displacing (-)-[3H]-nicotine from brain homogenates. Nevertheless, a direct comparison of (+)-[3H]-nicotine and (-)-[3H]-nicotine binding shows that the latter has a KD three times lower than the former. (-)-[3H]-Nicotine is bound to the greatest degree in hypothalamus and hippocampus, areas that also exhibited the most stereoselectivity for nicotine. However, differences in the binding affinities of the two isomers were far less than the pharmacological stereospecificity observed.
Advances in Experimental Medicine and Biology, 1993
1. Adv Exp Med Biol. 1993;335:21-8. Consequences of opiate-dependency in a monkey model of AIDS. ... more 1. Adv Exp Med Biol. 1993;335:21-8. Consequences of opiate-dependency in a monkey model of AIDS. Donahoe RM, Byrd LD, McClure HM, Fultz P, Brantley M, Marsteller F, Ansari AA, Wenzel D, Aceto M. Dept. of Psychiatry, Emory Univ., Atlanta, GA 30306. ...
Buspirone (CAS 36505-84-7) was evaluated in three animal models which were designed to study stag... more Buspirone (CAS 36505-84-7) was evaluated in three animal models which were designed to study stages of drug abuse most likely associated with compulsive abuse. Buspirone attenuated abrupt withdrawal in rhesus monkeys maximally-dependent on morphine. In addition, it completely blocked the emergence of cocaine-induced stereotyped behavior in rats and attenuated the hyperarousal or rausch syndrome in morphine-dependent and non-dependent rhesus monkeys. Buspirone was active at doses which caused little, if any, impairment in the animals. The results suggest that buspirone may possibly find application in the pharmacotherapy of opioid and cocaine abuse.
ABSTRACT Cocaine and pipradrol facilitated the avoidance performance of rats in Skinner boxes. Wh... more ABSTRACT Cocaine and pipradrol facilitated the avoidance performance of rats in Skinner boxes. When the drugs were withdrawn performance deteriorated to levels shown by rats that had never been drugged. The drugs seemed to temporarily affect either emotionality or activity rather than to permanently affect learning. Tricyanoaminopropene did not affect performance.
Nicotine produced antinociception in mice which was antagonized noncompetitively by naloxone. In ... more Nicotine produced antinociception in mice which was antagonized noncompetitively by naloxone. In addition, at significantly lower doses, nicotine noncompetitively antagonized morphine-induced antinociception. A speculative suggestion regarding the opiatergic and anti-opiatergic actions of nicotine is that it significantly promotes and maintains smoking behavior.
Journal of comparative and physiological psychology, 1968
... JACK PEARL, MARIO D. ACETO, AND JOHN J. FITZGERALD Sterling-Winthrop Research Institute, Rens... more ... JACK PEARL, MARIO D. ACETO, AND JOHN J. FITZGERALD Sterling-Winthrop Research Institute, Rensselaer, New York Pipradol and cocaine ... stimulants improve the avoidance performance of rats when in-jections are given before testing: ampheta-mines (Hearst & Whalen ...
Writhing was produced in mice by injecting them intraperitoneally with phenylquinone either 10 or... more Writhing was produced in mice by injecting them intraperitoneally with phenylquinone either 10 or 20 min before the start of scoring. The activity of two antiwrithing agents was compared: morphine and nalorphine at doses of 0.5 and 2.0 mg/kg injected subcutaneously 10, 20, or 40 min before scoring. Analyses of both quantal and graded data indicated that the antiwrithing activity
Mice were given a drug per os and 2 h later were challenged with an intravenous LD95 of nicotine.... more Mice were given a drug per os and 2 h later were challenged with an intravenous LD95 of nicotine. Amitriptyline, imipramine, doxepin, meprobamate, chlordiazepoxide, diazepam, trifluoroperazine, haloperidol, thioridazine, chlorpromazine, phenobarbital, propranolol and diphenylhydantoin were all active in protecting mice from extensor convulsions and lethality. Iproniazid, tranylcypromine, atropine, benztropine and trimethadione were inactive. There appears to be a relationship between blockage of nicotine-induced extensor convulsions and lethality in mice and sedative-antianxiety effects in man. This relationship is especially good for drugs designated antidepressant, antianxiety and antipsychotic.
Each of the dynorphin A(1-13) or dynorphin (dyn) treatment groups receiving naloxone showed a sig... more Each of the dynorphin A(1-13) or dynorphin (dyn) treatment groups receiving naloxone showed a significant overall reduction of overt signs compared with the dyn controls. The data suggested that the overt psychomotor effects of dyn in the rhesus monkey were especially prone to blockade by naloxone, and probably involved opioid mechanisms.
The resolution of racemic nicotine to provide optically pure (+)-nicotine and the synthesis of ra... more The resolution of racemic nicotine to provide optically pure (+)-nicotine and the synthesis of radiolabeled nicotine with high specific activity have facilitated the study of nicotine binding in brain. The actions of the stereoisomers of nicotine on the central nervous system are qualitatively similar in most tests but (-)-nicotine is more potent than the unnatural (+)-isomer by 10-fold or greater. Binding of radiolabeled nicotine to brain has both saturable and nonsaturable components. Only saturable binding is affected by incubation conditions such as time, temperature, pH and ion concentration. Excess concentrations of the stereoisomers are equally effective in displacing (-)-[3H]-nicotine from brain homogenates. Nevertheless, a direct comparison of (+)-[3H]-nicotine and (-)-[3H]-nicotine binding shows that the latter has a KD three times lower than the former. (-)-[3H]-Nicotine is bound to the greatest degree in hypothalamus and hippocampus, areas that also exhibited the most stereoselectivity for nicotine. However, differences in the binding affinities of the two isomers were far less than the pharmacological stereospecificity observed.
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