<i>In vivo</i> properties of SB 200646A, a 5‐HT<sub>2C/2B</sub> receptor antagonist

Kennett, Guy A.; Wood, Martyn; Glen, A.I.M.; Grewal, Savraj; It, Forbes; Gadre, A.; Blackburn, Thomas P.

doi:10.1111/j.1476-5381.1994.tb14808.x

Cited by 181 publications

(114 citation statements)

References 40 publications

(43 reference statements)

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“…The anxiogenic-like effects of mCPP in the social interaction test are prevented by the 5-HT2C/2B receptor antagonist, SB 200646A (Kennett et al, 1994) and by less selective antagonists of these sites (Kennett et al, 1989). The effects of mCPP in the elevated x-maze have at the present time only been reversed by less selective antagonists of the 5-HT2c/2B receptors (Gibson et al, 1994).…”

Section: Effectsmentioning

confidence: 99%

“…In man, these can be blocked by ritanserin, methysergide and metergoline, non-selective antagonists of the 5-HT2c receptor (see Kennett, 1993). In rats, anxiogenic-like effects of mCPP are prevented by SB 200646A (Kennett et al, 1994), the first 5-HT2C/2B receptor antagonist with selectivity over the 5-HT2A site (Forbes et al, 1993). Furthermore, SB 200646A alone has anxiolytic-like properties in animal models (Kennett et al, 1994;1995, Bill et al, 1995.…”

Section: Introductionmentioning

confidence: 99%

“…In rats, anxiogenic-like effects of mCPP are prevented by SB 200646A (Kennett et al, 1994), the first 5-HT2C/2B receptor antagonist with selectivity over the 5-HT2A site (Forbes et al, 1993). Furthermore, SB 200646A alone has anxiolytic-like properties in animal models (Kennett et al, 1994;1995, Bill et al, 1995. mCPP is also a potent agonist of the 5-HT2B receptor (Clineschmidt et al, 1985 and at present, all high affinity antagonists of the 5-HT2c receptor, including SB 200646A (Kennett et al, 1994), are equipotent at the 5-HT2B site (see Baxter et al, 1995).…”

Section: Introductionmentioning

confidence: 99%

“…Furthermore, SB 200646A alone has anxiolytic-like properties in animal models (Kennett et al, 1994;1995, Bill et al, 1995. mCPP is also a potent agonist of the 5-HT2B receptor (Clineschmidt et al, 1985 and at present, all high affinity antagonists of the 5-HT2c receptor, including SB 200646A (Kennett et al, 1994), are equipotent at the 5-HT2B site (see Baxter et al, 1995). It is therefore conceivable that the effects of mCPP and of SB 200646A are mediated by activity at the 5-HT2B receptor.…”

Section: Introductionmentioning

confidence: 99%

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Effects of the 5‐HT_2B receptor agonist, BW 723C86, on three rat models of anxiety

Kennett

Bright

Trail

et al. 1996

British J Pharmacology

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1 BW 723C86 (3 and 10 mg kg-', s.c. 30 min pretest), a 5-HT2B receptor agonist, increased total interaction, but not locomotion in a rat social interaction test, a profile consistent with anxiolysis. 2 The effect of BW 723C86 in the social interaction test is likely to be 5-HT2B receptor-mediated as it was prevented by pretreatment with the 5-HT2C,2B receptor antagonist, SB 200646A, (1 and 2 mg kg-', p.o., 1 h pretest) which did not affect basal levels of social interaction at the doses used. 3 An anxiolytic-like action was also observed in the rat Geller-Seifter conflict test, where BW 723C86 (0.5-50 mg kg-', s.c. 30 min pretest) modestly, but significantly increased punished, but not unpublished responding. 4 In a rat 5 min elevated x-maze test, BW 723C86 (1-10 mg kg-', s.c.) had no significant effect. 5 The maximal anxiolytic-like effect of BW 723C86 approached that of the benzodiazepine anxiolytic, chloradiazepoxide (5 mg kg-', s.c. 30 min pretest) in the social interaction test, but was markedly less in the Geller-Seifter test. The effect of BW 723C86 was also clearly less than chlordiazepoxide in the elevated x-maze procedure where it had no significant effect. 6 In conclusion, BW 723C86 exerted an appreciable anxiolytic-like profile in a rat social interaction test, but had a weaker effect in the Geller-Siefter and was ineffective in the elevated x-maze test used. These effects are likely to be 5-HT2B receptor-mediated.

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Section: Effectsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Effects of the 5‐HT_2B receptor agonist, BW 723C86, on three rat models of anxiety

Kennett

Bright

Trail

et al. 1996

British J Pharmacology

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106

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“…The model combines assessment of eating microstructural variables using the Sussex Ingestion Pattern Monitor (Yeomans 1996) alongside measures of emotional processing using the P1vital ® Oxford Emotional Test Battery (ETB) (Harmer et al 2004Murphy et al 2008). We examined the effect of a compound that has been reported to alter food intake and moodrelated behaviour in rodents, the preferential 5-HT2C receptor agonist metachlorophenylpiperazine (mCPP) (Kitchener and Dourish 1994;Kennett et al 1994;Hewitt et al 2002). The anorectic effects of mCPP in humans have been reported previously Sargent et al 1997) but detailed effects of this compound on appetite have yet to be 6 investigated.…”

mentioning

confidence: 99%

Effects of the 5-HT2C receptor agonist meta-chlorophenylpiperazine on appetite, food intake and emotional processing in healthy volunteers

et al. 2014

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(250 words)Rationale: The treatment of obesity is an increasing global health priority yet few effective drug treatments are currently available. The discovery of novel anti-obesity therapies could be assisted by the validation of experimental (translational) medicine models in healthy volunteers that assess efficacy and safety at an early stage of drug development. Objectives:To examine the effects of the 5-HT2C receptor agonist meta-chlorophenylpiperazine (mCPP) in an experimental medicine model assessing both appetite and mood. Methods: Using a between-subjects double blind placebo controlled design, 24 male and 24 female participants were randomly assigned to either placebo, 15mg or 30mg mCPP treatment groups. Lunch was eaten from a Universal Eating Monitor (UEM) that measured eating rate and participants completed the P1vital ® Oxford Emotional Test Battery (ETB) and a series of appetite and mood ratings. Results: mCPP reduced appetite, and in females, enhanced measures of satiation. The drug also enhanced memory for emotional material in the word recall and recognition memory tasks of the ETB. Conclusions: The results provide new insight into the effects of mCPP on appetite, satiety and memory in humans. In addition, our data provide an illustration of the value of measuring changes in appetite and mood in healthy volunteers to determine the potential efficacy and safety of novel anti-obesity drugs.

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Pharmacological actions of the atypical antipsychotic drug clozapine: A review

Ashby

Wang

1996

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165

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Clozapine [8-chloro- 11-(4-methyl- 1-piperazinyl)-3H-dibenzo (b,e)(1,4) diazepine], or clozaril, is a member of the dibenazepine class of antipsychotic drugs. Initially, studies in animals using a number of neurochemical, biochemical, electrophysiological, and behavioral paradigms indicated that clozapine was markedly different from various typical antipsychotic drugs such as haloperidol and chlorpromazine. Subsequently, clinical studies have shown that clozapine is effective in ameliorating the core symptoms, as well as the negative symptoms, in schizophrenia. However, clozapine has a much lower propensity for inducing neurological side effects after acute or repeated administration compared to various typical neuroleptics. Furthermore, clozapine is therapeutically effective in treating about 30% of schizophrenic patients who are resistant to standard antipsychotic drugs. Based on the above information, clozapine has been designated an atypical antipsychotic drug. However, at this time, it is not entirely clear why clozapine is such a unique antipsychotic drug. To date, there has not been a comprehensive review regarding clozapine's pharmacological profile. Therefore, we will review clozapine's profile in the following areas: 1) affinity for neurotransmitter receptors in the brain; 2) electrophysiology (in vivo, single-cell recording and iontophoresis; in vitro studies); 3) in vivo microdialysis and voltammetry; 4) monoamine turnover or metabolism; 5) intermediate early gene expression; 6) positron emission tomography studies; and 7) molecular biological studies. We will also compare and contrast clozapine's acute and chronic effects, and discuss the merits of various hypotheses that have been put forward to explain clozapine's unique profile.

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In vivo properties of SB 200646A, a 5‐HT_2C/2B receptor antagonist

Cited by 181 publications

References 40 publications

Effects of the 5‐HT_2B receptor agonist, BW 723C86, on three rat models of anxiety

Effects of the 5‐HT_2B receptor agonist, BW 723C86, on three rat models of anxiety

Effects of the 5-HT2C receptor agonist meta-chlorophenylpiperazine on appetite, food intake and emotional processing in healthy volunteers

Pharmacological actions of the atypical antipsychotic drug clozapine: A review

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In vivo properties of SB 200646A, a 5‐HT2C/2B receptor antagonist

Cited by 181 publications

References 40 publications

Effects of the 5‐HT2B receptor agonist, BW 723C86, on three rat models of anxiety

Effects of the 5‐HT2B receptor agonist, BW 723C86, on three rat models of anxiety

Effects of the 5-HT2C receptor agonist meta-chlorophenylpiperazine on appetite, food intake and emotional processing in healthy volunteers

Pharmacological actions of the atypical antipsychotic drug clozapine: A review

Contact Info

Product

Resources

About

In vivo properties of SB 200646A, a 5‐HT_2C/2B receptor antagonist

Effects of the 5‐HT_2B receptor agonist, BW 723C86, on three rat models of anxiety

Effects of the 5‐HT_2B receptor agonist, BW 723C86, on three rat models of anxiety