Effect of zotepine on fenfluramine-induced hyperthermia in rats.

Satoh, Hisashi; Fujiwara, Tatsujiro; Mori, Jo; Shimomura, Kyoichi; Ono, Takaharu; Kikuchi, Hiroyuki

doi:10.1254/jjp.34.261

Cited by 6 publications

(1 citation statement)

References 6 publications

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“…Our present data are in line with the receptor binding profile of ZOT (Meltzer et al, 1989;Kanba et al, 1991) and other behavioral studies (Uchida et al, 1979;Shimomura et al, 1982; Pharmacological EjJects 0/Zotepine and other Antipsychotics on the Central 5-HTz Receptors Pharmacopsychiat. 26 (1993) 57 Satoh et al, 1984), which regard ZOT as a potent antagonist of central 5-HT2 receptors.…”

Section: Discussionmentioning

confidence: 99%

Pharmacological Effects of Zotepine and other Antipsychotics on the Central 5-HT₂Receptors

Czyrak

Jaros²,

Moryl³

et al. 1993

Pharmacopsychiatry

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The effects of the atypical neuroleptic zotepine in comparison with clozapine, risperidone and haloperidol were examined in tests related to the central 5-HT2 activity. Zotepine, as well as clozapine and risperidone, were very potent inhibitors of the 5-HTP-induced head twitches (the behavior mediated by 5-HT2 receptors) in mice, with rank order of potency risperidone > zotepine > clozapine; haloperidol used in high doses only slightly reduced the effect of 5-HTP. Zotepine, clozapine, risperidone and haloperidol antagonized the stimulatory effects of mCPP on the hind limb flexor reflex in spinal rats. As the mCPP-induced stimulation is considered to be mediated by 5-HT2 receptors, the above results provide further evidence for the 5-HT2 antagonistic activity of the drugs studied. Te rank order of potency in that test was the same as in the 5-HTP-induced head twitches (risperidone > zotepine > clozapine). The effect of haloperidol was somewhat unspecific, since its active doses were very high. In the model of hind limb flexor reflex of spinal rats, the anti-alpha 2-adrenergic effect was also tested. Clonidine-induced stimulation of the hind limb flexor reflex (an alpha 2-adrenergic effect) was antagonized by zotepine, clozapine, risperidone and haloperidol. It may be concluded that zotepine, clozapine and risperidone show an alpha 2-adrenergic antagonistic activity (order of potency: zotepine = risperidone > clozapine). The effect of haloperidol may be considered unspecific, since it is observed at high (cataleptic) doses only. In conclusion, it appears that zotepine, as well as clozapine and risperidone, are strong 5-HT2 antagonists, while haloperidol is not.

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Section: Discussionmentioning

confidence: 99%

Pharmacological Effects of Zotepine and other Antipsychotics on the Central 5-HT₂Receptors

Czyrak

Jaros²,

Moryl³

et al. 1993

Pharmacopsychiatry

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The place of dibenzo[b,f]thiepin derivatives in medicinal chemistry: Structures and activities

Protiva

1996

Journal of Heterocyclic Chem

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Erratum to: Zotepine: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in the management of schizophrenia

Prakash¹,

Lamb²

1998

CNS Drugs

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Effect of zotepine on fenfluramine-induced hyperthermia in rats.

Cited by 6 publications

References 6 publications

Pharmacological Effects of Zotepine and other Antipsychotics on the Central 5-HT₂Receptors

Pharmacological Effects of Zotepine and other Antipsychotics on the Central 5-HT₂Receptors

The place of dibenzo[b,f]thiepin derivatives in medicinal chemistry: Structures and activities

Erratum to: Zotepine: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in the management of schizophrenia

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Effect of zotepine on fenfluramine-induced hyperthermia in rats.

Cited by 6 publications

References 6 publications

Pharmacological Effects of Zotepine and other Antipsychotics on the Central 5-HT2Receptors

Pharmacological Effects of Zotepine and other Antipsychotics on the Central 5-HT2Receptors

The place of dibenzo[b,f]thiepin derivatives in medicinal chemistry: Structures and activities

Erratum to: Zotepine: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in the management of schizophrenia

Contact Info

Product

Resources

About

Pharmacological Effects of Zotepine and other Antipsychotics on the Central 5-HT₂Receptors

Pharmacological Effects of Zotepine and other Antipsychotics on the Central 5-HT₂Receptors