Antagonism of hypothermia and behavioral response to apomorphine: A simple, rapid and discriminating test for screening antidepressants and neuroleptics

Puech, Alain J.; Chermat, R; Poncelet, Marc; Doaré, L; Simon, Pierre

doi:10.1007/bf00433508

Cited by 90 publications

(44 citation statements)

References 11 publications

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“…Inhibition of hypothennia induced by high dose apomorphine is also a frequently used method for detecting antidepressant activity and EGYT-4201 proved to be effective in this model as well. However, its potency did not reach that of other antidepressants cited in the literature [Puech et al, 1981;Pawlowski and Mazela, 19861. The compound was also active in potentiation of the effect of L-dopa and D-amphetamine, although it showed only moderate activity.…”

Section: Discussionmentioning

confidence: 89%

Psychopharmacological effects of an imino‐thiazolidine derivative antidepressant candidate, EGYT‐4201

Gyertyán

Petöcz

Szikora

et al. 1991

Drug Development Research

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The imino-thiazolidine derivative EGYT-4201 exhibited marked activity in pharmacological tests characteristic for antidepressants. In the behavioral despair model and in antagonizing the effect of tetrabenazine its efficacy was considerably higher than that of several tricyclic and second generation antidepressant drugs. The compound also proved to be active in inhibiting the hypothermic effect of apomorphine. It potentiated the lethal effect of yohimbine, the hypermotility provoked by L-dopa, and the stereotypy induced by D-amphetamine. In contrast to amitriptyline and nomifensine, EGYT-4201 showed neither sedative nor stimulant actions on spontaneous and conditioned behavior. The compound, similar to amitriptyline and viloxazine, exerted a moderate anticonvulsive effect against pentylenetetrazole, bicuculline, and picrotoxin. EGYT-4201 did not exhibit significant anticholinergic activity on physostigmine induced lethality, oxotremorine evoked tremor, and isolated guinea pig ileum. In acute toxicity studies it proved to be more favourable than the reference compounds. EGYT-4201 did not inhibit the enzymatic activity of the monoamino-oxidase (MAO) enzyme, nor did it block the uptake of monoamines. The molecule was found to be inactive in binding studies of noradrenergic, dopaminergic, and serotonergic receptor types.

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Section: Discussionmentioning

confidence: 89%

Psychopharmacological effects of an imino‐thiazolidine derivative antidepressant candidate, EGYT‐4201

Gyertyán

Petöcz

Szikora

et al. 1991

Drug Development Research

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“…At noradrenergic terminals apomorphine acting through D 2 receptors prevents noradrenaline release. Puech et al (1981) showed that hypothermia induced by high doses of apomorphine is antagonized by antidepressants. Different animal models often require different doses of the same drug, in order to show any effect.…”

Section: Discussionmentioning

confidence: 99%

“…Apomorphine treatment causes a decrease in the rectal temperature and this effect is prevented by antidepressive drugs such as imipramine (Puech et al, 1981). In order to confi rm a possible antidepressive effect of the H. pectinata AE, we tested the effects of apomorphine in rectal temperature of mice treated with the plant AE.…”

Section: Apomorphine-induced Hypothermiamentioning

confidence: 99%

Effects of the aqueous extract from Hyptis pectinata leaves on rodent central nervous system

Bueno¹,

Moreira²,

Silva³

et al. 2006

Rev. bras. farmacogn.

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RESUMO: "Efeitos do extrato aquoso das folhas da Hyptis pectinata sobre o sistema nervoso central de roedores". Neste trabalho foram estudados os efeitos do extrato aquoso (EA) obtido das folhas da Hyptis pectinata sobre o sistema nervoso central de roedores. Os seguintes modelos experimentais foram utilizados em camundongos, machos e fêmeas, da linhagem Wistar: "screening" farmacológico, campo aberto, nado forçado, hipotermia induzida por apomorfi na, labirinto em cruz elevado e tempo de sono induzido por tiopental. O extrato foi administrado por via oral em dose única, 30 minutos antes de cada teste. No "screening" farmacológico o EA (400 mg/kg, p.o., n = 3) diminuiu a freqüência do comportamento de auto-limpeza. No teste do campo aberto o EA diminuiu o tempo gasto em auto-limpeza (AE400: 51,3 ± 8,8, q = 5,513, P < 0.01, n = 10) de maneira similar ao diazepam (control: 107,3 ± 14,2; diazepam: 15,4 ± 4,3, q = 9,049, P < 0.001, n = 10). No teste do nado forçado o EA (400 mg/kg) diminuiu o tempo de imobilidade (con: 181,3 ± 7,2 s; imip: 91,6 ± 8,9 s, q = 7,958, P < 0,001; AE400: 111,6 ± 14,5 s, q = 6,193, P < 0,001, n = 9) indicando um possível efeito antidepressivo. Isto foi confi rmado no modelo de hipotermia induzida pela apomorfi na onde o EA (200 mg/kg) antagonizou o efeito da apomorfi na (AE200: -0,27 o C, q = 5,588, P < 0,001, n = 10) de maneira similar à imipramina (5 mg/kg) (control: -1,08 o C; imipramine: 0,02 o C, q = 7,589, P < 0,001, n = 10). Nenhum efeito do EA foi observado nos testes do labirinto em cruz elevado e do tempo de sono induzido por tiopental. Nossos resultados sugerem um possível efeito antidepressivo do extrato aquoso obtido das folhas da Hyptis pectinata. Unitermos:Hyptis pectinata, Lamiaceae, plantas medicinais, depressão. ABSTRACT:The effects of the aqueous extract (AE) from Hyptis pectinata leaves was studied on rodent central nervous system (CNS). Pharmacological screening, open fi eld, forced swimming, apomorphine-induced hypothermia, elevated plus maze and thiopental-induced sleep tests were used in male and female Swiss mice and Wistar rats. The AE was admnistered orally in single doses 30 minutes before each test. In the screening test the AE (400 mg/kg, p.o., n =3) decreased the frequency of grooming behavior. In the open fi eld test it decreased the amount of time rats spent grooming (AE400: 51.3 ± 8.8, q = 5.513, P < 0.01, n = 10), similarly to diazepam (control: 107.3 ± 14.2; diazepam: 15.4 ± 4.3, q = 9.049, P < 0.001, n = 10). In the forced swimming test the AE (400 mg/kg) decreased the immobility time (con: 181.3 ± 7.2 s; imip: 91.6 ± 8.9 s, q = 7.958, P < 0.001; AE400: 111.6 ± 14.5 s, q = 6.193, P < 0.001, n = 9), indicating a possible antidepressive effect. This was confi rmed in the apomorphine-induced hypothermia model where the extract (200 mg/kg) antagonized the apomorphine effect (AE200: -0.27 o C, q = 5.588, P < 0.001, n = 10), similarly to imipramine (imipramine: 5 mg/kg) (control: -1.08 o C; imipramine: 0.02 o C, q = 7.589, P < 0.001, n = 10). No effect of the...

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“…With regard to the effects of these infusions on the hypothermia induced by high-dose apomorphine (16 mg/kg s.c.), none of the infusions showed a significant decrease of the hypothermia induced by the drug compared with the control (Table 4), at variance with the standard drug imipramine. Nevertheless, H. grandifolium infusion antagonized (but not significantly) in 30% of mice the hypothermia induced by apomorphine 30 and 60 min after administration, indicating a possible inhibition of norepinephrine reuptake (Puech et al, 1981).…”

Section: Antidepressant Activitymentioning

confidence: 98%

Evaluation of the central properties of several Hypericum species from the Canary Islands

Prado¹,

Rabanal²,

Sánchez-Mateo³

2002

Phytotherapy Research

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The infusions of the aerial parts in blossom of Hypericum canariense, H. glandulosum, H. reflexum and H. grandifolium (Hypericaceae) were evaluated for their pharmacological activity on the central nervous system in mice using various behavioural models including locomotor and muscle relaxant activity, effect on normal body temperature, pentobarbital-induced sleep, oxotremorine and tetrabenazine-induced syndrome, apomorphine-induced hypothermia and 5-hydroxytryptophan-induced head twitches, as well as a forced swimming test. These infusions did not alter significantly the locomotor activity, pentobarbital induced sleeping time and body temperature, with the exception of H. canariense which produced a slight but significant hypothermia. Additionally, no muscle relaxant or anticholinergic activity were observed. These infusions antagonized the ptosis and/or motor depression induced by tetrabenazine as well as shortening the immobility time in the forced swimming test. The observations suggest that the infusions of these Hypericum species possess antidepressant activity in mice, without inducing muscle relaxation, anticholinergic and sedative properties.

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Antagonism of hypothermia and behavioral response to apomorphine: A simple, rapid and discriminating test for screening antidepressants and neuroleptics

Cited by 90 publications

References 11 publications

Psychopharmacological effects of an imino‐thiazolidine derivative antidepressant candidate, EGYT‐4201

Psychopharmacological effects of an imino‐thiazolidine derivative antidepressant candidate, EGYT‐4201

Effects of the aqueous extract from Hyptis pectinata leaves on rodent central nervous system

Evaluation of the central properties of several Hypericum species from the Canary Islands

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