Adrenergic Neurone-blocking Agents related to Choline 2,6-Xylyl Ether Bromide (TM 10), Bretylium and Guanethidine

Boura, A. L. A.; Copp, F. C.; Green, A. F.; Hodson, H. F.; Ruffell, G. K.; Sim, M.F.; Walton, Edward; Grivsky, E. M.

doi:10.1038/1911312a0

Cited by 39 publications

(7 citation statements)

References 3 publications

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“…The ability of aralkylguanidines, such as N-benzyl-N'N'-dimethylguanidine, to cause adrenergic neurone blockade has been previously reported (Boura, Copp, Green, Hodson, Ruffell, Sim, Walton & Grivsky, 1961;Boura & Green, 1963). However, little has been published on aralkylguanidines in which only one of the amino-nitrogen atoms is substituted.…”

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confidence: 99%

Adrenergic Neurone Blocking Activity of Some Aralkylguanidines

Fielden¹,

Green²,

Willey³

1965

British Journal of Pharmacology and Chemotherapy

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confidence: 99%

Adrenergic Neurone Blocking Activity of Some Aralkylguanidines

Fielden¹,

Green²,

Willey³

1965

British Journal of Pharmacology and Chemotherapy

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“…Each, however, has certain disadvantages, tolerance being prominent with the first and the onset and offset of action slow with the second, while undesirable side-effects commonly occur with each. The search for an ideal hypotensive drug continues and a series of compcunds related to bretylium and guanethidine was described by Boura, Copp, Green, Hodson, Ruffell, Sim, Walton & Grivsky (1961), the most potent of these being bethanidine.…”

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The Effects of Bethanidine on the Peripheral Circulation in Man

Fewings

Hodge

Scroop

et al. 1964

British Journal of Pharmacology and Chemotherapy

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Bethanidine has been administered intra-arterially and intravenously into normotensive subjects and its effects on the limb blood vessels, arterial blood pressure, vascular sensitivity to noradrenaline and the degree and time course of sympathetic nerve blockade have been studied. The drug caused an initial constriction of hand and forearm vessels which is attributed to release of catechol amines since it is abolished by the prior administration of phenoxybenzamine. The constriction was followed by a sustained vasodilatation lasting between 5 and 20 hr. Sympathetic blockade of hand vessels commenced immediately on infusion and was complete within 1 hr of administration. Recovery occurred in about 5 hr. Sensitivity to intra-arterial noradrenaline was increased within 10 to 15 min of infusion and before sympathetic blockade was complete. Intravenous administration caused a slight rise in blood pressure of supine subjects. Baroreceptor reflex responses of heart and of limb vessels elicited by tilting the subject feet downwards were abolished by bethanidine and postural hypotension occurred. Bethanidine is a potent sympathetic blocking agent in man with properties intermediate between those of bretylium and guanethidine.

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“…Willey (1957) demonstrated that the depressor effect of small doses of xylocholine in the anaesthetized cat may be attributed to a muscarinic action. Boura et al (1961) have also attributed muscarinic properties to the guanidino congener of xylocholine, that is SK&F 70418. Examination of this compound in vitro did, in fact, reveal some stimulation of the isolated ileum of the guinea-pig, but this was inhibited by methanthelinium bromide only at concentrations far in excess of those required to antagonize the specific muscarinic effects of acetylcholine.…”

Section: Discussionmentioning

confidence: 99%

“…In an attempt to prepare compounds having a specific adrenergic neurone blocking activity with a rapid onset and a short duration of action while being devoid of parasympathomimetic activity, the xylyloxyethyl chain of xylocholine was combined with the guanidino-group of guanethidine. The resulting compound, N-[2-(2,6-xylyloxy)ethyl]guanidine sulphate (SK&F 70418), showed marked adrenergic neurone blocking activity (Boura, Copp, Green, Hodson, Ruffell, Sim, Walton & Grivsky, 1961;Barron, Bavin, Durant, Natoff, Spickett & Vallance, 1963). The pharmacology of this compound is reported below.…”

mentioning

confidence: 99%