Pharmacological properties of AF 1161, a new psychotropic drug

Silvestrini, Bruno; Cioli, V.; Burberi, S; Catanese, B

doi:10.1016/0028-3908(68)90069-5

Cited by 76 publications

(18 citation statements)

References 11 publications

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“…The pA2 values (Schild, 1957) were found for trazodone, a psychoactive drug known to have a potent anti-5-hydroxytryptaminergic action (Silvestrini, Cioli, Burberi & Catanese, 1968;Domino, 1973), and for amitriptyline which blocks noradrenaline and 5-HT uptake in the brain (Carlsson, Corroli, Fuke & Hokfelt, 1969). A further comparison of the responses to 5-HT in the stomach and uterus was made using methysergide.…”

Section: Introduction Methodsmentioning

confidence: 99%

Heterogeneity of 5‐hydroxytryptamine receptors in the rat uterus and stomach strip

Wrigglesworth

1983

British J Pharmacology

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1 Experiments were performed using the rat isolated uterus and the rat stomach strip to investigate the effects of 5-hydroxytryptamine (5-HT) on 5-HT receptors in the presence of different antagonists. Amitriptyline, methysergide and trazodone were used to antagonize the response to 5-HT in these tissues. 2 The pA2 value for amitriptyline with 5-HT as the agonist was estimated from the Schild plot analysis and found to differ significantly (P<0.05) in the stomach strip (6.36) from that in the isolated uterus (9.06). 3 A similar difference was found using trazodone; here the pA2 value was 6.74 in the stomach strip and 8.49 in the isolated uterus. 4 These results indicate a difference between the two tissues. This difference is discussed in terms of heterogeneity of 5-HT receptors.

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Section: Introduction Methodsmentioning

confidence: 99%

Heterogeneity of 5‐hydroxytryptamine receptors in the rat uterus and stomach strip

Wrigglesworth

1983

British J Pharmacology

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“…Previous experiments have shown that bendazac and hydrocortisone have super imposible antinflammatory effects only in conditions where the vascular response is pre minent, while the former is superior against necrotic responses, the latter is superior against proliferative responses (1). Results of these experiments confirm that bendazac and hy drocortisone possess a different spectrum of effects.…”

Section: Discussionmentioning

confidence: 52%

Topical Activity of Bendazac on Experimental Burns

Barcellona

Silvestrini

1971

Jpn.J.Pharmacol

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Bendazac or 1-benzyl-indazole 3-oxyacetic acid is a topical antinflammatory drug which in previous experiments was shown to preferentially inhibit inflammatory processes progressing towards necrosis (1). This activity has been temptatively related to a pre vention of protein denaturation (2-4).The aim of these experiments was to study effects of bendazac and hydrocortisone on heat-induced burns and on acetic acid-induced erythema. Two differently formulated creams have been investigated, in an attempt to find out the most suitable one for topical uses. METHODSCFI mice and Wistar rats of both sexes, weighing 20-30 and 130-170 g respectively, were used. The skin areas to be treated were clipped with an electric shaver. When not otherwise indicated, animals were kept under urethane anesthesia (1.7 g/kg i.p. in rats and 1.5 g/kg i.p. in mice) throughout the whole experiment.Burns were produced in rats by putting on the abdomen for 30 seconds a test tube (weighing 50 g and with a diameter of about 8 mm) in which water was circulated at a temperature of 70°C. In each animal two burns were produced, one on the upper third and the other on the lower third of the abdomen. Two minutes later, the burnt areas were rubbed gently with 2 ml of the creams under investigation. One hour later, the ani mals were intravenously injected with 1 ml of a water solution containing 0.5% Evans Blue and 0.9% NaC1. Two hours after application of the creams, animals were killed by a blow on the head and the burnt skin was stretched and inserted between two glass slides. The intensity of blueing, resulting from accumulation of Evans Blue in the injured skin, was estimated by a Joyce Loebl mod. II photodensitometer devised for automatic read ing of electrophoretic tracings.Acetic acid erythema was studied in mice. A disc of filter paper, 4 mm in diameter, was soaked with glacial acetic acid and applied on the back of animals taking care that the paper adhered to the skin. After 15 seconds the disc was removed, the excess of acetic acid was wiped and a minute later 0.5 ml of the creams were applied locally. One hour later, the animals were intravenously injected with 0.5 ml of a water solution containing 0.1 % Evans Blue and 0.9 % NaC1. After 30 minutes animals were killed by a blow on

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“…In the case of acetic acid-induced erythema and heat-induced burns the original values were transformed into a percentage of the highest response according to a previ ously described method (2).…”

Section: Methodsmentioning

confidence: 99%

Topical Anti-Inflammatory Effects of Af 2071: A Comparative Study With Bendazac and Corticosteroids, Both Alone and Associated

Feo

Cioli

Putzolu

1975

Japanese Journal of Pharmacology

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Abstract-Bendazac has anti-inflammatory effects which are different from or com plementary to those of corticosteroids; therefore, it has been associated with hydro cortisone or dexamethasone, in the attempt to obtain a dermatological preparation with a wide range of therapeutic applications. Results in laboratory animals were discouraging, in that a diminished activity was observed. On the other hand, bend acort or (pregn-4ene 3, 20 dione 11j3, 17a, 21 trihydroxy, 21 ester with acetic acid

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Pharmacological properties of AF 1161, a new psychotropic drug

Cited by 76 publications

References 11 publications

Heterogeneity of 5‐hydroxytryptamine receptors in the rat uterus and stomach strip

Heterogeneity of 5‐hydroxytryptamine receptors in the rat uterus and stomach strip

Topical Activity of Bendazac on Experimental Burns

Topical Anti-Inflammatory Effects of Af 2071: A Comparative Study With Bendazac and Corticosteroids, Both Alone and Associated

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