The action of dazopride to enhance gastric emptying and block emesis

Costall, B.; Domeney, A.M.; Gunning, Simon J.; Kelly, M.E.; Naylor, R.J.; Nohria, Virinder; Owera-Atepo, J.B.; Simpson, K.M.; Tan, Connie C.W.; Tattersall, David

doi:10.1016/0028-3908(87)90227-9

Cited by 15 publications

(1 citation statement)

References 18 publications

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“…Drugs used to increase gastric emptying are believed to act on gastric emptying through an antagonist effect on both central (Peringer et al, 1976) and peripheral dopamine receptors . In contrast, other studies have indicated that the antagonism of dopamine receptors is not a prerequisite for the gastrointestinal action of pro-motility drugs (Bateman, 1985(Bateman, , 1986Costall et al, 1987). Furthermore, the findings suggested an important role of a-adrenoceptors in the regulation of gastric emptying in man.…”

Section: Discussionmentioning

confidence: 73%

The effect of phentolamine on basal and pethidine‐induced inhibition of gastric emptying in healthy volunteers.

Petring

1989

Brit J Clinical Pharma

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1. The effect of phentolamine 5 mg i.v. on basal and pethidine‐induced inhibition of gastric emptying of semisolid TC‐99m labelled Chelex‐100 resin/oatmeal was studied in ten healthy volunteers. 2. Each volunteer acted as his/her own control. 3. Basal gastric emptying remained unchanged after administration of phentolamine. 4. Administration of phentolamine reversed the pethidine‐induced inhibition of gastric emptying.

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Section: Discussionmentioning

confidence: 73%

The effect of phentolamine on basal and pethidine‐induced inhibition of gastric emptying in healthy volunteers.

Petring

1989

Brit J Clinical Pharma

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The Ferret in Nausea and Vomiting Research: Lessons in Translation of Basic Science to the Clinic

Sert¹,

Andrews²

2014

Biology and Diseases of the Ferret

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New Alkoxypyridine‐sulfonamides: Synthesis, Biological Evaluation, and Physicochemical Properties

Liégeois

Dive

Dupont

et al. 1991

Helvetica Chimica Acta

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As a further pharmacomodulation of benzamide derivatives, two structural modifications were introduced by synthesizing pyridincsulfonamides 5 and 6 (Scheme). The pharmacological profile of substituted benzamides such as metoclopramide (2) is not retained in the pyridine-sulfonamides 6 : the latter have very low toxicity but do not exhibit any affinity for D2 and 5-HT2 receptors, and gastrointestinal prokinetic activity is weak (Table 3 ) . Lipophilicity does not seem to be a determining factor for this lack of activity. A conformational analysis shows that the sulfonamide group in 6 is rather unfavorable for an intramolecular H-bond formation when compared to the carboxamide group of, c.g., 2. Nevertheless, the interaction remains possible and leads to a stable conformation (Fig. 1, Table 5 ) . Moreover, the sp3 character of the sulfonamide N-atom of 6 modifies the relative spatial orientation of one substituent in relation to each of the others. This feature seems to be more important for the observed very low activity than the H-bond formation itself.

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The action of dazopride to enhance gastric emptying and block emesis

Cited by 15 publications

References 18 publications

The effect of phentolamine on basal and pethidine‐induced inhibition of gastric emptying in healthy volunteers.

The effect of phentolamine on basal and pethidine‐induced inhibition of gastric emptying in healthy volunteers.

The Ferret in Nausea and Vomiting Research: Lessons in Translation of Basic Science to the Clinic

New Alkoxypyridine‐sulfonamides: Synthesis, Biological Evaluation, and Physicochemical Properties

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