Substituted benzamides, antagonists

Many DA receptor antagonists (neuroleptics) for treating psychoses (for example, schizophrenia) have become efficient medicines. However, most of them induce severe extrapyramidal side-effects (EPS) akin to parkinsonian symptoms and also, more seriously, they induce tardive dyskinesias (TD). There is a need for improvements in the neuroleptics in the clinic. The substituted benzamides are D2 antagonists, some of which display a high degree of limbic selectivity. Such a regional selectivity has been suggested to be beneficial from the side-effects point of view [11,12]. 

Substituted benzamides include metodopramide (discussed previously) and trimethobenzamide. Their primary mechanism of antiemetic action is believed to be dopamine-receptor blockade. Trimethobenzamide also has weak antihistaminic activity. For prevention and treatment of nausea and vomiting, metodopramide may be given in the relatively high dosage of 10-20 mg orally or intravenously every 6 hours. The usual dose of trimethobenzamide is 250 mg orally, 200 mg rectally, or 200 mg by intramuscular injection. The principal adverse effects of these central dopamine antagonists are extrapyramidal restlessness, dystonias, and parkinsonian symptoms. 

Because of the wide range of specificity of sulpiride and other substituted benzamides, it is possible to administer these drugs intravenously and differentiate renal or mesenteric vasodilation produced by DA from non-specific vasodilating agents such as bradykinin (18,Jj)). However, we disagree with Shepperson et al 20) who estimated the relative potency of less specific antagonists by the intravenous route. 

Tiapride is a substituted benzamide related to sulpiride, a selective dopamine D2 and D3 receptor antagonist with little propensity for causing catalepsy and sedation. It has... 

Batanopride is a substituted benzamide with 5-HT3 receptor antagonist activity. It is claimed to be free of dopaminergic properties. Clinical studies have concentrated on its use in patients suffering severe vomiting as a result of cytostatic therapy, but have run into problems because of poor tolerance at effective doses. The most important dose-limiting adverse effect is severe hypotension (1) but diarrhea and electrocardiographic changes also occur. 

Clebopride [inn. usan] (cleboprlde n-ialate [jan]) is a substituted benzamide, a (Dj) DOPAMINE RECEPTOR ANTAGONIST, and has activity as a visceral ANTISPASMODIC and antinauseant and antiemetic. 

SUltopride [inn] (sultopride hydrochloride [jan] LIN 1418) is one of the substituted benzamides, with properties similar to sulpiride, and is a dopamine receptor antagonist. It has ANTIEMETIC actions, and has been used as an antipsychotic in the management of acute psychosis, sultopride hydrochloride sultopride. 

Substituted benzamide Glucocorticoid muscarinic receptor antagonist... 

Substituted benzamide Hj receptor antagonist, glucocorticoid, benzodiazepine... 

The pyrrolizine ring found only in new compounds related to substituted benzamides SC53116 and its racemic mixture SC49518, lead to potent and highly effective 5-HT4 agonists devoid of potent 5-HTg antagonistic properties [28, 29]. 

OSalmid [inn, jan] (L171 8 and many other names) is a benzamide and has been used as a CHOLERETIC AGENT, osanetant [inn] (SR 142801) is a substituted piperidinyl-methylacetamide. a TACHYKININ RECEPTOR ANTAGONIST selective for the NKs-receptor subtype. 

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