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1. The regional penetration into the brain of exogenous labelled noradrenaline (following unilateral injection into the internal carotid artery) was correlated with the effect of this amine on regional cerebral blood flow as measured by the [14C]ethanol technique in anaesthetized rats. 2. A hyperosmolar solution of urea was injected into the ipsilateral internal carotid artery to induce osmotic opening of the blood-brain barrier. 3. The extent of the blood-brain barrier damage was followed by macroscopic and fluorescence microscopic visualization of systemically injected Evans blue, and by the determination of the brain uptake index for noradrenaline. 4. The extravasation of Evans blue was restricted to the brain areas nourished by the internal carotid artery on the same side as the injection. 5. The normally low penetration of noradrenaline into the brain was enhanced fourfold in those brain regions that showed Evans blue extravasation following the administration of hypertonic urea. 6. In the same regions, the systemic administration of noradrenaline markedly increased local cerebral blood flow, compared to the contralateral hemisphere that was unaffected by the injection of urea. This effect on regional cerebral blood flow was blocked by the beta-receptor antagonist, propranolol.

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