Partial agonist effect of 2-[2-(1,4-Benzodioxanyl)]-2-imidazoline (RX 781094) at presynaptic ?2-adrenoceptors in rabbit ear artery

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Abstract
Summary Ear arteries from rabbits were preincubated with3H-noradrenaline and then perfused. 2-[2-(1,4-Benzodioxanyl)]-2-imidazoline (RX 781094) 0.1 or 1μM reduced the overflow of3H-noradrenaline and total tritium elicited by 13 electrical pulses at 0.25 Hz or 26 pulses at 0.5 Hz. RX 781094 1 μM increased the overflow elicited by 52 pulses at 1 Hz. The inhibitory effects were blocked by yohimbine 10 μM but not by prazosin 1 μM. The alleged antagonist RX 781094 possesses intrinsic activity at the presynaptic α2-autoreceptor of the ear artery.