European Journal of Pharmacology, 145 (1988) 227-230 227
Elsevier
EJP 20051
Short communication
Ketanserin antagonises the anorectic effect of DL-fenfluramine in the rat
Graeme Hewson *, Glynis E. Leighton, Raymond G. Hill and John Hughes
Parke-Davis Research Unit, Addenbrookes Hospital Site, Hills Road, Cambridge CB2 2QB, U.K.
Received 9 November 1987, accepted 10 November 1987
To determine the role played by 5-HT 2 receptors in the anorectic action of DL-fenfluramine, the ability of the
selective 5-HT2 receptor antagonist ketanserin to block the reduction in food intake produced by this drug was
investigated in non-deprived rats. Ketanserin (1 and 2.5 mg/kg i.p.) produced a dose-dependent antagonism of the
anorectic effect of DL-fenfluramine (3 mg/kg i.p.). Prazosin (1 mg/kg i.p.) did not antagonise this effect. It is
concluded that the anorectic actions of DL-fenfluramine are mediated via 5-HT2 receptors.
Ketanserin; Prazosin; DL-Fenfluramine anorexia
1. Introduction
DL-Fenfluramine is an anorectic agent used
clinically in the treatment of obesity. Although its
precise mechanism of action remains unclear, it is
generally accepted that fenfluramine exerts its
anorectic activity by selectively enhancing sero-
toninergic mechanisms in the brain (Garattini et
al., 1986). In support of such a mechanism,
antagonists at 5-hydroxytryptamine (5-HT) recep-
tors, such as methysergide and metergoline, have
been shown to attenuate the reductions in food
intake produced by fenfluramine (Barrett and Mc-
Sharry, 1975; Carruba et al., 1986).
Recently, three subtypes of 5-HT receptor have
been defined, based on the use of selective
antagonists (Bradley et al., 1986). The present
study investigated the effect of the selective 5-HT 2
receptor antagonist ketanserin (Leysen et al., 1981)
on the reduction in food intake produced by DL-
fenfluramine. As ketanserin can also block al-
adrenoceptors (Fozard, 1982), the effects of the
* To whom all correspondence should be addressed.
selective cq-adrenoceptor antagonist prazosin on
the anorectic action of DL-fenfluramine was also
determined.
2. Materials and methods
2.1. Animals
Male Hooded Lister rats (Olac, starting weight
175-200 g) were used. They were housed individu-
ally at a constant room temperature (21 ° C) and
maintained on a 12 h light : 12 h dark cycle (lights
on 07:00 h).
2.2 Drugs
Ketanserin tartrate (Janssen) and DL-fen-
fluramine hydrochloride (Sigma) were dissolved in
distilled water. Prazosin hydrochloride (Pfizer) was
dissolved in 0.01 N tartaric acid (final pH of
solution 4-5). All drugs were injected i.p. in a
volume of 1 ml/kg. Doses refer to the weight of
free base.
0014-2999/88/$03.50 © 1988 Elsevier Science Publishers B.V. (Biomedical Division)