Adrenoceptors presently are classified into three main subclasses: alpha1-, alpha2-, and beta-receptors, each with three (perhaps more) subtypes. All three alpha1-adrenoceptor subtypes are present in rat brain. The purpose of this review is to assess the role of alpha1-adrenoceptors in the modulation of synaptic transmission and plasticity, as well as their ability to modulate higher cerebral functions, such as attentional and memory processes. However, since there are no truly subtype-specific agonists or antagonists available at present, it is virtually impossible to allocate a particular central effect to one or other of the subtypes. The activation of alpha1-adrenoceptors reduces the firing probability and glutamate release in the cornu ammonis of the hippocampus. Alpha1-Adrenoceptors may flexibly modulate weak and strong activation of the pyramidal neurones in the neocortex. Alpha1-Adrenoceptors play only a minor role in the modulation of long-term potentiation in the hippocampus, and may influence many brain functions also via non-neuronal mechanisms. since glial cells can express alpha1-adrenoceptors. At the behavioural level, the activation of alpha1-adrenoceptors promotes vigilance and influences working memory and behavioural activation, while having only a minor role in the modulation of long-term memory.