Receptor heterogeneity for bombesin-like peptides in the rat central nervous system

International Union of Pharmacology. LXVIII. Mammalian Bombesin Receptors: Nomenclature, Distribution, Pharmacology, Signaling, and Functions in Normal and Disease States

“…Binding studies and studies of biological activity provide evidence for BB 1 on both gastrointestinal and urogenital smooth muscle cells (von Schrenck et al, 1989;Severi et al, 1991;Bitar and Coy, 1992;Kim et al, 1993). Binding studies have confirmed the widespread distribution of BB 1 in the brain showing especially high levels in the olfactory tract of the rat (Ladenheim et al, 1990(Ladenheim et al, , 1992(Ladenheim et al, , 1993a.…”

“…Binding studies have confirmed the widespread distribution of BB 2 receptors in the brain, showing high levels in the cortex as well as the suprachiasmatic and supraoptic nuclei of the rat (Ladenheim et al, 1990(Ladenheim et al, , 1992(Ladenheim et al, , 1993aMoody and Merali, 2004). Binding studies and studies of biological activity provide evidence for BB 2 receptors on both gastrointestinal and urogenital smooth muscle cells (Severi et al, 1991;Kilgore et al, 1993;Ladenheim et al, 1997a;Milusheva et al, 1998;ter Beek et al, 2004;Fleischmann et al, 2005).…”

“…Numerous classes of selective BB 2 receptor antagonists were developed before the cloning of the BB 1 , and these also confirmed the presence of the BB 1 on esophageal smooth muscle (von Schrenck et al, 1990). After the pharmacologic description of BB 1 on esophageal muscle and before its cloning in 1991, by use of selective BB 2 receptor antagonists or binding studies with radiolabeled NMB and selective agonists or BB 2 receptor antagonists, BB 1 receptors were demonstrated in the CNS (Ladenheim et al, 1990) and on gastric smooth muscle cells (Severi et al, 1991).…”

“…Once the receptors were defined using binding studies, cross-linking studies, and studies of biological activity (Kris et al, 1987;Sinnett-Smith et al, 1988;Tache et al, 1988;von Schrenck et al, 1989;Huang et al, 1990;Ladenheim et al, 1990;Lebacq-Verheyden et al, 1990), an active effort to clone the GRP-R was undertaken by Dr. Eliot Spindel, Oregon Regional Primate Center, and Dr. James Battey, National Institutes of Health. In 1990 using electrophysiological and luminometric Xenopus oocyte expression assays, Spindel et al (1990) succeeded in cloning the GRP-R from murine Swiss 3T3 cells, which express high levels of this receptor (Rozengurt, 1988).…”

“…Binding studies and the development of highly selective antagonists established unequivocally the existence of two different classes of receptors in mammalian tissues mediating the actions of these peptides (Jensen et al, 1978;Moody et al, 1978;Jensen and Gardner, 1981;Coy et al, 1988;von Schrenck et al, 1989von Schrenck et al, , 1990Ladenheim et al, 1990;Jensen and Coy, 1991;Metz et al, 1992). One class had a high affinity for GRP and a lower affinity for NMB (termed GRP-R, GRP receptor, or GRP-preferring receptor) and the other class had a higher affinity for NMB than for GRP (termed NMB-R, NMB receptor, or NMB-preferring receptor) (Jensen and Gardner, 1981;Moody et al, 1988Moody et al, , 1992von Schrenck et al, 1989von Schrenck et al, , 1990Ladenheim et al, 1990Ladenheim et al, , 1992Wang et al, 1992). Subsequently, two mammalian receptors with high affinity for GRP (Spindel et al, 1990; or NMB have been cloned in addition to a closely related orphan receptor (Gorbulev et al, 1992;Fathi et al, 1993b) and one related receptor from amphibians (Nagalla et al, 1995), which will be discussed in more detail below (Table 1).…”