Comparative Investigations of Terguride Isomers on Central Dopamine and Noradrenaline Functions
Terguride is an 8α-ergoline derived from the dopamine (DA) receptor agonist lisuride. In previous neuropharmacological (Wachtel and Dorow, 1983) and neurobiochemical (Kehr, 1984) experiments terguride has been shown to exhibit a profile of action which characterises the compound as a DA partial agonist. Thus, at normosensitive central DA receptors the DA antagonistic component of action prevails (Wachtel and Dorow, 1983) whereas the DA agonistic component of action becomes evident at non-synaptic DA receptors like those located on pituitary lactotrophs (Wachtel and Dorow, 1983; Wachtel et al., 1984a) or is unmasked at supersensitive central DA receptors as judged from the release of contralateral rotations in rats bearing unilateral nigrostriatal lesions (Dlabac and Krejci, 1980), the production of stereotypies and hyperlocomotion in chronically reserpinised rats (Wachtel et al., 1984b) or the release of contralateral rotations in hemiparkinsonian 1methy-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated monkeys (Brücke et al., 1988). The DA partial agonism of terguride might also contribute to reducing the incidence of unwanted side effects like nausea and emesis being associated with the use of DA agonists in man (Wachtel and Dorow, 1983).
KeywordsStereotyped Behaviour Partial Agonistic Activity Automatic Registration Central Dopamine Contralateral Rotation
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- Brücke, T., Danielczyk, W., Simanyi, M., Sofic, E. and Riederer, P., 1986, Terguride: Partial dopamine agonist in the treatment of Parkinson’s disease, Adv. Neurol., 45: 573–576.Google Scholar
- Crossley, D.I., 1984, The effects of idazoxan, an a2-adrenoceptor antagonist in depression - a preliminary investigation, Abstr. 9th IUPHAR Congress, London 1724 P.Google Scholar
- Dallabonzana, D., Liuzzi, A., Oppizzi, G., Cozzi, R., Verde, G., Chiodini, P., Rainer, E., Dorow, R. and Horowski, R., 1986, Chronic treatment of pathological hyperprolactinemia and acromegaly with the new ergot derivative terguride, J. Clin. Endocrinol. Metab., 63: 1002–1007.PubMedCrossRefGoogle Scholar
- Dlabac, A. and Krejci, I., 1980, Central dopaminergic effects of ergoline derivatives, Activ. Nerv. Sup., 22: 208–209.Google Scholar
- Horowski, R., 1978, A new method for automatic registration of stereotyped behaviour in the rat, Arzneimittelforsch., 12: 2281–2286.Google Scholar
- Santamaria, J., Tolosa, E.S., Vallés, A., Bayes, A., Blesa, R. and Masana, J., 1986, Mental depression in untreated Parkinson’s disease of recent onset, Adv. Neurol., 45: 443–446.Google Scholar
- Suchy, I., Rinne, U.K. and Wachtel, H., 1986, Evaluation of terguride in patients with Parkinson’s disease, Adv. Neurol., 45: 577–581.Google Scholar