Detail of "6190-39-2"

Reference

Pharmaceutical preparation of ergot alkaloids

Pharmaceutical preparation of ergot alkaloids. (Sandoz-Patent G.m.b.H., Ger.). Ger. Offen. DE 2546577 21 Apr 1977, 8 pp. (German). (Germany). CODEN: GWXXBX. CLASS: IC: A61K031-48. APPLICATION: DE 75-2546577 17 Oct 1975. DOCUMENT TYPE: Patent CA Section: 63 (Pharmaceuticals) New galenic formulations for ergot alkaloids comprise the alkaloid or one of its synthetic derivs., hydrates or salts, and a polyalkylene glycol and/or polyvinylpyrrolidone [9003-39-8] and/or vinyl acetate-vinylpyrrolidone copolymer. For example, 34.6 g dihydroergotamine methanesulfonate (I) [6190-39-2] and 195.4 g polyvinylpyrrolidone were heated in 500 mL MeOH at 60.degree. at give a clear soln. The MeOH was evapd., and the dry residue was ground, and can be used in prepg. tablets, capsules or pills.

A comparison of pre- and postsynaptic effects of

A comparison of pre- and postsynaptic effects of .alpha.-adrenolytic drugs in the pulmonary artery of the rabbit. Borowski, E.; Starke, K.; Ehrl, H.; Endo, T. (Pharmakol. Inst., Univ. Essen, Essen, Ger.). Neuroscience, 2(2), 285-96 (English) 1977. CODEN: NRSCDN. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Strips of the main pulmonary artery of the rabbit were preincubated with [3H]noradrenaline and then superfused and elec. stimulated transmurally. Yohimbine-HCl [65-19-0], dihydroergotamine methanesulfonate [6190-39-2], and tolazine-HCl [59-97-2] at low concns. enhanced the stimulation-evoked overflow of tritium; up to one hundred times higher concns. were needed in order to reduce stimulation-evoked contractions. Piperoxan-HCl [135-87-5] and mianserine-HCl [21535-47-7] enhanced the evoked overflow and reduced the evoked contractions at identical concns. Phentolamine-HCl [73-05-2], azapetine phosphate [130-83-6], clozapine [5786-21-0] and phenoxybenzamine-HCl [63-92-3] at low concns. diminished the contractile response; up to thirty times higher concns. were needed to increase the evoked overflow of tritium. At high concns., all drugs accelerated basal tritium outflow. Sepn. of individual [3H]-compds. revealed that a high concn. of piperoxan markedly accelerated the basal outflow of [3H]3,4-dihydroxyphenylglycol. Lower concns. of piperoxan and yohimbine that did not affect the basal efflux of [3H]-compds. greatly increased the evoked overflow of [3H]noradrenaline as well as of [3H]3,4-dihydroxyphenylglycol and [3H]normetanephrine. The pulmonary artery contains postsynaptic .alpha.-adrenoceptors which mediate smooth muscle contractions. Its noradrenergic neurones possess presynaptic .alpha.-receptors which mediate inhibition of the per pulse release of noradrenaline by a neg. feedback mechanism. .alpha.-Adrenolytic drugs vary widely in their relative pre- and postsynaptic effects. Yohimbine, dihydroergotamine and tolazoline preferentially block presynaptic .alpha.-receptors and a low concns. selectively facilitate noradrenaline release. Phentolamine, azapetine, clozapine and phenoxybenzamine preferentially block postsynaptic .alpha.-receptors and at low concns. selectively antagonize the contractile response. Piperoxan and mianserin occupy an intermediate position. In a given tissue, pre- and postsynaptic .alpha.-receptors may differ in their structure.