Vasoactive intestinal receptor

Melatonin [73-31-4] C 2H N202 (31) has marked effects on circadian rhythm (11). Novel ligands for melatonin receptors such as (32) (12), C2yH2gN202, have affinities in the range of 10 Af, and have potential use as therapeutic agents in the treatment of the sleep disorders associated with jet lag. Such agents may also be usehil in the treatment of seasonal affective disorder (SAD), the depression associated with the winter months. Histamine (see Histamine and histamine antagonists), adenosine (see Nucleic acids), and neuropeptides such as corticotropin-like intermediate lobe peptide (CLIP) and vasoactive intestinal polypeptide (VIP) have also been reported to have sedative—hypnotic activities (7). 

Pituitary Adenylyl Cyclase-activating Polypeptide (PACAP) is a 38-amino acid peptide (PACAP-38), which is widely expressed in the central nervous system. PACAP is most abundant in the hypothalamus. It is also found in the gastrointestinal tract, the adrenal gland and in testis. Its central nervous system functions are ill-defined. In the periphery, PACAP has been shown to stimulate catecholamine secretion from the adrenal medulla and to regulate secretion from the pancreas. Three G-protein coupled receptors have been shown to respond to PACAP, PAQ (PACAP type I) specifically binds PACAP, VPACi and VPAC2 also bind vasoactive intestinal peptide (VDP). Activation of PACAP receptors results in a Gs-mediated activation of adenylyl cyclase. 

Laburthe, M., Breant, B., and Rouyer-Fessard, C. (1984) Molecular identification of receptors for vasoactive intestinal peptide in rat intestinal epithelium by covalent cross-linking. Eur. J. Biochem. 139, 181-187. 

Wood, C.L., and O Dorisio, M.S. (1985) Covalent cross-linking of vasoactive intestinal polypeptide to its receptors on intact human lymphoblasts./. Biol. Chem. 260, 1243-1247. 

Carrero I, Femandez-Moreno MD, Perez-Albarsanz MA, et al. 1989. Lindane effect upon the vasoactive intestinal peptide receptor-effector system in rat enterocytes. Biochem Biophys Res Comm 159(3) 1391-1396. 

Figure 2.8. Scheme of a chimeric peptide with examples for each of the distinct domains. 0X26, anti-rat transferrin receptor monoclonal antibody (mAh) 84-15, anti-human insulin receptor mAh cHSA, cationized human serum albumin VIP, vasoactive intestinal polypeptide DALDA, dermorphin analogue NGF, nerve growth factor BDNF, brain-derived neurotrophic factor PNA, peptide nucleic acid (3-gal, (3-galactosidase. 

BDNF, brain derived neurotrophic factor CBF, cerebral blood flow GDNF, glial cell line derived neurotrophic factor NGF, nerve growth factor TfR, transferrin receptor VIP, vasoactive intestinal polypeptide. 

Cutler DJ, Haraura M, Reed HE, et. al 2003 The mouse VPAC2 receptor confers suprachiasmatic nuclei cellular rhythmicity and responsiveness to vasoactive intestinal polypeptide in vitro. Eur J Neurosci. 17 197—204 Ebling FJ 1996 The role of glutamate in the photic regulation of the suprachiasmatic nucleus. Prog Neurobiol 50 109-132... 

Stimulation of 5-HT4 receptors on the presynaptic terminal of submucosal intrinsic primary afferent nerves enhances the release of their neurotransmitters, including calcitoningene-related peptide, which stimulate second-order enteric neurons to promote the peristaltic reflex (Figure 62-4). These enteric neurons stimulate proximal bowel contraction (via acetylcholine and substance P) and distal bowel relaxation (via nitric oxide and vasoactive intestinal peptide). 

The heterogeneity of dopaminergic neurons may also be judged by the fact that the cotransmitter systems involving dopamine and peptides are varied in the central nervous system. For example, in the corpus striatum, in addition to dopamine, acetylcholine, y-aminobutyric acid, serotonin, glutamate, and aspartate, one also finds peptides such as enkephalin, substance P, somatostatin, neuropeptide Y, cholecystokinin, neurotensin, and vasoactive intestinal peptide. Although many neuroleptics block dopamine receptors, they may have selective effects on the peptides and other parts of the brain. A few examples will be cited. 

Wei Y, Mojsov S. Tissue specific expression of different human receptor types for pituitary adenylate cyclase activating polypeptide and vasoactive intestinal polypeptide implications for their role in human physiology. J Neuroendocrinol 1996 8 811-817. 

Usdin TB, Bonner TI, Mezey E. Two receptors for vasoactive intestinal polypeptide with similar specificity and complementary distributions. Endocrinology 1994 135 2662-2680. 

Jimenez-Anguiano A, Garcia-Garcia F, Mendoza-Ramirez JL, Duran-Vazquez A, Drucker-Colin R. Brain distribution of vasoactive intestinal peptide receptors following REM sleep deprivation. Brain Res 1996 728 37-46. 

Bourgin P, Ahnaou A, Laporte AM, Hamon M, Adrien J. Rapid eye movement sleep induction by vasoactive intestinal peptide infused into the oral pontine tegmentum of the rat may involve muscarinic receptors. Neuroscience 1999 89 291-302. 

Correia-de-Sd P, Timdteo MA, Ribeiro JA (2001) Synergism between A2A-adenosine receptor activation and vasoactive intestinal peptide to facilitate [3H]-acetylcholine release from the rat motor nerve terminals. Neurosci Lett 309 101 —4... 

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