The mechanism of action of 2‐halogenoethylamines at the adrenergic α‐receptor and a further investigation of the “spare receptor” hypothesis

J. F. MORAN, Christopher Triggle, D. J. TRIGGLE

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24 Citations (Scopus)

Abstract

The evidence for “spare‐receptors” has been examined in the adrenergic α‐receptor system of the rat vas deferens using N‐(2‐bromoethyl)‐N‐ethyl‐l‐naphthylmethylamine (SY.28) and NN‐dimethyl‐2‐phenylethylamine hydrobromides as the antagonist species. It is clearly demonstrated that “spare‐receptors” are not present in this tissue and that the observed parallel shift of the dose‐response curve of noradrenaline produced by SY.28 is due to a competitive reversible phase of action of the corresponding ethyleneimine species rather than to the presence of “spare‐receptors”. Additionally, these experiments have revealed the existence of a significant non‐competitive reversible phase of action of SY.28. From radiochemical studies and the observed first order recovery of tissue response following blockade by NN‐dimethyl‐2‐bromo‐2‐phenylethylamine, it is concluded that the α‐receptors in the rat vas deferens are indistinguishable from the α‐receptors in the rabbit aorta in their behaviour towards this agent. From these results and those of others, it may be concluded that there is no existing evidence for “spare receptors” in adrenergic α‐receptor systems. 1969 Royal Pharmaceutical Society of Great Britain

Original languageEnglish
Pages (from-to)38-46
Number of pages9
JournalJournal of Pharmacy and Pharmacology
Volume21
Issue number1
DOIs
Publication statusPublished - 1969
Externally publishedYes

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Vas Deferens
Adrenergic Receptors
Aorta
Norepinephrine
Rabbits
aziridine

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

Cite this

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abstract = "The evidence for “spare‐receptors” has been examined in the adrenergic α‐receptor system of the rat vas deferens using N‐(2‐bromoethyl)‐N‐ethyl‐l‐naphthylmethylamine (SY.28) and NN‐dimethyl‐2‐phenylethylamine hydrobromides as the antagonist species. It is clearly demonstrated that “spare‐receptors” are not present in this tissue and that the observed parallel shift of the dose‐response curve of noradrenaline produced by SY.28 is due to a competitive reversible phase of action of the corresponding ethyleneimine species rather than to the presence of “spare‐receptors”. Additionally, these experiments have revealed the existence of a significant non‐competitive reversible phase of action of SY.28. From radiochemical studies and the observed first order recovery of tissue response following blockade by NN‐dimethyl‐2‐bromo‐2‐phenylethylamine, it is concluded that the α‐receptors in the rat vas deferens are indistinguishable from the α‐receptors in the rabbit aorta in their behaviour towards this agent. From these results and those of others, it may be concluded that there is no existing evidence for “spare receptors” in adrenergic α‐receptor systems. 1969 Royal Pharmaceutical Society of Great Britain",
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