Adrenergic Neurone Blocking Activity of Some Aralkylguanidines

The Effects of Some Aralkylguanidines in Mice

“…3. These results suggested that, as happens in cats (Fielden et al, 1965), the (+)-isomer was antagonizing the adrenergic neurone blockade due to the (-)-isomer. This was confirmed directly by giving the (+)-isomer (20 mg/kg) before a normally highly active dose (20 mg/kg) of the (-)-isomer, when virtually no ptosis was produced.…”

Optical Isomers of Β‐hydroxyphenethylguanidine: Effects on Heart Noradrenaline and on Sympathetic Blockade

“…As shown in Table 2 both isomers reduced the relaxation caused by the potent adrenergic, neurone blocking drug (-)-N-(1-phenylethyl)guanidine (Fielden, Green & Willey, 1965). The (+)-isomer was the more active.…”

“…The preparation of 83-hydroxyphenethylguanidine sulphate and its optical isomers (Green, Fielden, Bartlett, Cozens, Eden & Hills, 1967), and of (-)-N-(l-phenylethyl)guanidine sulphate, N-[l-(2,4-xylyl)ethyl] guanidine sulphate and N-benzyl-N-methylguanidine sulphate (Fielden, Green & Willey, 1965) have been previously described. Other drugs were obtained commercially.…”

A COMPARATIVE STUDY OF THE NORADRENALINE‐DEPLETING AND SYMPATHETICBLOCKING ACTIONS OF GUANETHIDINE AND (—)‐β‐HYDROXYPHENETHYLGUANIDINE

“…The pressor response to tyramine was, however, markedly reduced. In the treated cat 0.5 mg/kg tyramine hydrochloride raised the blood pressure by only 20 mm Hg, whereas in an untreated cat 0.25 mg/kg caused (Fielden, Green & Willey, 1965); N-benzyl-N-methylguanidine, an antagonist to adrenergic neurone blockade (Fielden & Green, 1966); and N-(p-methoxy-a-methylphenethyl)guanidine, which has little effect on adrenergic transmission but which is a moderately active monoamine-oxidase inhibitor (Fielden & Green, 1965a). Depletion by reserpine is, in contrast, little affected by amphetamine or by N-benzyl-N-methylguanidine.…”