This article investigates the distribution of neurotransmitters, neuropeptides, and related receptors in the vestibular nuclei complex (VNC) of the adult rat by means of immunohistochemistry, in situ hybridization, and quantitative receptor autoradiography. The entire complex proves to be rich in muscarinic receptors and it shows a high density of imipramine and benzodiazepine binding sites. Peptidergic neurons and a few positive fibers are described in the caudal part of the VNC. In particular, the medial vestibular nucleus contains a number of neurons expressing both the enkephalin mRNA and peptide. This nucleus and the lateral vestibular nucleus are also rich in opiate receptors. Substance P, thyrotropin releasing hormone, and neurotensin receptors are also found in the medial and in the spinal vestibular nuclei. In spite of the presence of alpha 2 catecholaminergic receptors, no thyrosine-hydroxylase-immuno-reactive elements are seen in the caudal VNC. The possible functional meaning of these data is discussed.