Abstract
The cataleptic and antistereotypic abilities of clozapine, sulpiride and thioridazine were determined in the rat and compared with the responses of typical neuroleptic agents, haloperidol, fluphenazine and pimozide. Haloperidol and fluphenazine caused a dose-dependent cataleptic state which attained maximum intensity: the effects of pimozide were also dose-dependent but, although the catalepsy was marked, maximum intensity was not attained. In contrast, thioridazine, clozapine and sulpiride each caused a very weak, but definite, cataleptic response although a dose-dependency could not be demonstrated. Pretreatment of animals with alpha-methylparatyrosine was shown to significantly potentiate the cataleptic actions of haloperidol, fluphenazine, pimozide, thioridazine and sulpiride but failed to modify the action of clozapine, Threshold cataleptic doses of all agents markedly synergised in the production of catalepsy with threshold doses of the cholinergic drug RS86. Similarly, all "neuroleptic" agents tested were shown to reduce the intensity of the stereotyped behaviour induced by amphetamine, apomorphine and nomifensine in a dose-dependent manner but only haloperidol, fluphenazine and pimozide were shown to be capable of 100% inhibition. The antistereotypic abilities of haloperidol, fluphenazine and pimozide were most marked against amphetamine, but this was not a consistent observation for thioridazine, clozapine and sulpiride. Threshold, or even subthreshold, doses of both the typical and atypical neuroleptic agents combined with threshold doses of RS86 markedly synergised in the antagonism of the stereotypic actions of amphetamine, apomorphine and nomifensine.
MeSH Terms
Animals
Apomorphine/antagonists & inhibitors
Behavior, Animal/drug effects
Catalepsy/chemically induced
Clozapine/pharmacology
Dextroamphetamine/antagonists & inhibitors
Dibenzazepines/pharmacology
Dose-Response Relationship, Drug
Drug Synergism
Fluphenazine/pharmacology
Haloperidol/pharmacology
Humans
Isoquinolines/antagonists & inhibitors
Male
Methyltyrosines/pharmacology
Pimozide/pharmacology
Rats
Spiro Compounds/pharmacology
Stereotyped Behavior/drug effects
Succinimides/pharmacology
Sulpiride/pharmacology
Thioridazine/pharmacology
Tranquilizing Agents
Chemicals
Dibenzazepines
Isoquinolines
Methyltyrosines
Spiro Compounds
Succinimides
Tranquilizing Agents
Pimozide
Sulpiride
Clozapine
Haloperidol
Apomorphine
Thioridazine
Fluphenazine
Dextroamphetamine
Authors & Affiliations
2 authors, click to expand affiliations / ORCID
Costall B
Naylor R J
References (22)
22 references, click to expand
-
Nomifensine: a potent dopaminergic agonist of antiparkinson potential.
Psychopharmacologia. 1975;41(2):153-64
PMID: 1098084
-
Parkinsonism and related phenomena from administration of drugs: their production and control under clinical conditions and possible relation to therapeutic effect.
Rev Can Biol. 1961 Jun;20:549-60
PMID: 13899798
-
Parkinson's disease: from brain homogenate to treatment.
Fed Proc. 1973 Feb;32(2):183-90
PMID: 4143953
-
Anti-muscarinic properties of neuroleptics and drug-induced Parkinsonism.
Nature. 1974 Apr 12;248(449):596-7
PMID: 4150951
-
Antischizophrenic drugs and brain cholinergic receptors. Affinity for muscarinic sites predicts extrapyramidal effects.
Arch Gen Psychiatry. 1974 Jul;31(1):58-61
PMID: 4152054
-
Effect of single and repeated administration of clozapine on the metabolism of dopamine and noradrenaline in the brain of the rat.
Eur J Pharmacol. 1974 Jul;27(2):180-90
PMID: 4152854
-
Neuroleptics: relation between cataleptic and anti-turning actions, and role of the cholinergic system.
J Pharm Pharmacol. 1974 Dec;26(12):981-4
PMID: 4156868
-
[An original psychotropic drug: sulpiride].
Sem Hop. 1969 Apr 20;45(19):1301-14
PMID: 4307000
-
Dopamine turnover in the corpus striatum and the lumbic system after treatment with neuroleptic and anti-acetylcholine drugs.
J Pharm Pharmacol. 1972 Nov;24(11):905-6
PMID: 4405656
-
[Neuropharmacological findings after chronic administration of haloperidol, loxapine and clozapine].
Arzneimittelforschung. 1974 Jul;24(7):981-3
PMID: 4408075
-
[Clinical-neuroleptic investigation of N-((1-ethyl-pyrrolidine-2-yl)-methyl)-2-methoxy-5-sulfamyl-benzamide-neuroleptic sulpiride (Dogmatil) in acutly ill schizophrenics].
Int Pharmacopsychiatry. 1974;9(2):77-94
PMID: 4603413
-
Mesolimbic involvement with behavioural effects indicating antipsychotic activity.
Eur J Pharmacol. 1974 Jun;27(1):46-58
PMID: 4604756
-
Stereotyped and circling behaviour induced by dopaminergic agonists after lesions of the midbrain raphe nuclei.
Eur J Pharmacol. 1974 Dec;29(2):206-22
PMID: 4613561
-
Effects of clozapine on cerebral catecholaminergic neurone systems.
Br J Pharmacol. 1972 Dec;46(4):736-40
PMID: 4676274
-
Neuroleptic and non-neuroleptic catalepsy.
Arzneimittelforschung. 1973 May;23(5):674-83
PMID: 4740210
-
Is there a relationship between the involvement of extrapyramidal and mesolimbic brain areas with the cataleptic action of neuroleptic agents and their clinical antipsychotic effect?
Psychopharmacologia. 1973;32(2):161-70
PMID: 4796282
-
[The influence of sulpiride on motor activity and vigilance in the mouse].
Pathol Biol. 1968 Jun-Jul;16(11):663-5
PMID: 4878601
-
Pimozide treatment of chronic schizophrenics as compared with haloperidol and penfluridol maintenance treatment. A multidisciplinary approach.
Acta Psychiatr Belg. 1972 Mar;72(2):199-214
PMID: 5056015
-
[Preliminary clinical experiences with sulpiride].
Nord Psykiatr Tidsskr. 1971;25(4):340-6
PMID: 5154118
-
The pharmacology of 8-chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepine (clozapine).
Farmaco Prat. 1971 Oct;26(10):603-25
PMID: 5157543
-
The prediction of sedative potency of neuroleptics.
Mod Probl Pharmacopsychiatry. 1970;5:47-50
PMID: 5527167
-
Is it possible to predict the clinical effects of neuroleptic drugs (major tranquillizers) from animal data? IV. An improved experimental design for measuring the inhibitory effects of neuroleptic drugs on amphetamine-or apomorphine-induced "Cheroing" and "agitation" in rats.
Arzneimittelforschung. 1967 Jul;17(7):841-54
PMID: 5632842