The present article provides a concise overview of progress in our understanding of neuropeptides, their receptors and the current and potential ways in which they may be targeted for clinical use. Neuropeptide systems offer certain characteristics that distinguish them from those utilizing classic neurotransmitters and thus make them increasingly attractive for drug targeting. A key example of the highly successful use of neuropeptide receptor ligands is that of opioid receptor agonists for the treatment of pain.
View Article and Find Full Text PDFVasodilatation in the dura mater has been implicated in migraine pathogenesis. Anti-migraine triptan drugs block vasodilatation by binding to 5-HT1B/1D receptors localized on the peripheral sensory terminals and dural blood vessel smooth muscles. Previous studies suggest that calcitonin gene-related peptide (CGRP) released from Adelta-fibres plays a more important role than substance P (SP) released from C-fibres in inducing dural vasodilatation and that one of the antimigraine mechanisms of triptan drugs is inhibiting CGRP release.
View Article and Find Full Text PDFBrain Res Mol Brain Res
March 2001
The precise involvement of 5-ht(5A), 5-ht(5B), 5-ht(6) and 5-HT(7) receptors in the pleiotropic actions of 5-HT remain incompletely known. To gain insights into their physiological function(s), localization of mRNAs encoding these subtypes was carried out using in situ hybridization on rat brain sections. Localization was heterogeneous.
View Article and Find Full Text PDFThe mammalian superior colliculus is an important subcortical integrator of sensorimotor behaviours. It is multi-layered, each layer containing specific neuronal types and possessing distinct input/output relationships. Here we use in situ hybridisation methods to map the distribution of seven neurotransmitters/neuromodulator systems in adult rat superior colliculus.
View Article and Find Full Text PDFThe bradykinin B1 receptor is thought to be induced by tissue injury and inflammation. In the present study, we have investigated whether there is a basal expression of B1 receptor in dorsal root ganglion (DRG) and trigeminal ganglion neurons in rats. A substantial number of neurons in both DRGs and trigeminal ganglia were found to be B1-immunoreactive in rats.
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