Diana E Hurlbut | Irvine Valley College (original) (raw)
Papers by Diana E Hurlbut
European Journal of Pharmacology, 1987
BAM 18 is a derivative of the opioid precursor proenkephalin A. Although it exists in rat and gui... more BAM 18 is a derivative of the opioid precursor proenkephalin A. Although it exists in rat and guinea-pig brain in relatively high concentrations, its physiological function is presently unknown. In the present study we have determined the opioid receptor selectivity of this peptide using radioligand binding and peripheral tissue bioassay. When selective binding conditions were used, BAM 18 bound to the # opioid receptor with an affinity three times that of the r opioid receptor and over 10 times that of the 8 opioid receptors (K i = 0.29, 0.75, and 3.2 nM respectively). BAM 18 also displayed mixed receptor selectivity in in vitro bioassay. K e values for naloxone antagonism of BAM 18 agonist activity in the electrically stimulated guinea-pig ileum and the mouse vas deferens were 4.3 and 9.9 nM, respectively. These data indicate that BAM 18 binds to all three opioid receptor subtypes with a selectivity profile of #>x>& BAM 18; Proenkephalin A; Metorphamide; Opioid peptides; Opioid receptors
Life Sciences, 1982
... Printed in the USA DIFFERENTIAL APPEARANCE OF OPIATE RECEPTOR SUBTYPES IN NEONATAL RAT BRAIN ... more ... Printed in the USA DIFFERENTIAL APPEARANCE OF OPIATE RECEPTOR SUBTYPES IN NEONATAL RAT BRAIN Frances M. Leslie, Sharleen Tso and Diana E. Hurlbut Department of Pharmacology College of Medicine University of California, Irvine Irvine, California 92717 ...
Developmental Brain Research, 1987
Recent studies have demonstrated that opioid receptors may be functional at early stages of ontog... more Recent studies have demonstrated that opioid receptors may be functional at early stages of ontogeny, and may modulate specific developmental functions. It is presently unknown, however, which particular opioid receptor subtype(s) may be involved. In the preent study, we have used selective radioligand binding conditions in combination with quantitative autoradiography to examine the ontogeny of g-, r-and ~-opioid receptors in the developing rat brain. Membrane binding data indicate that the affinities of#-, r-and 6sites for radiolabeled drugs are similar in neonatal and adult rats. g-And r-receptors are present in significant densities during early neonatal periods, while h-receptors appear much later. Autoradiographic data indicate that #-and r-receptors appear early in the development of several brain regions, including the neostriatum, olfactory tubercle and rostral midbrain, and later in other regions such as the thalamus and hypothalamus. Whereas the densities of r-binding sites remain relatively constant throughout development, there is a transient appearance and/or redistribution of#-receptors in several brain areas. &Receptors are present in low densities in the basal forebrain at birth. The level of h-receptor binding increases markedly during the third postnatal week in all brain areas examined. The early appearance of#-and r-receptors during the ontogeny of the brain suggests that these receptors, at least in part, mediate the developmental actions of exogenous and endogenous opioids.
European Journal of Pharmacology, 1987
BAM 18 is a derivative of the opioid precursor proenkephalin A. Although it exists in rat and gui... more BAM 18 is a derivative of the opioid precursor proenkephalin A. Although it exists in rat and guinea-pig brain in relatively high concentrations, its physiological function is presently unknown. In the present study we have determined the opioid receptor selectivity of this peptide using radioligand binding and peripheral tissue bioassay. When selective binding conditions were used, BAM 18 bound to the # opioid receptor with an affinity three times that of the r opioid receptor and over 10 times that of the 8 opioid receptors (K i = 0.29, 0.75, and 3.2 nM respectively). BAM 18 also displayed mixed receptor selectivity in in vitro bioassay. K e values for naloxone antagonism of BAM 18 agonist activity in the electrically stimulated guinea-pig ileum and the mouse vas deferens were 4.3 and 9.9 nM, respectively. These data indicate that BAM 18 binds to all three opioid receptor subtypes with a selectivity profile of #>x>& BAM 18; Proenkephalin A; Metorphamide; Opioid peptides; Opioid receptors
Life Sciences, 1982
... Printed in the USA DIFFERENTIAL APPEARANCE OF OPIATE RECEPTOR SUBTYPES IN NEONATAL RAT BRAIN ... more ... Printed in the USA DIFFERENTIAL APPEARANCE OF OPIATE RECEPTOR SUBTYPES IN NEONATAL RAT BRAIN Frances M. Leslie, Sharleen Tso and Diana E. Hurlbut Department of Pharmacology College of Medicine University of California, Irvine Irvine, California 92717 ...
Developmental Brain Research, 1987
Recent studies have demonstrated that opioid receptors may be functional at early stages of ontog... more Recent studies have demonstrated that opioid receptors may be functional at early stages of ontogeny, and may modulate specific developmental functions. It is presently unknown, however, which particular opioid receptor subtype(s) may be involved. In the preent study, we have used selective radioligand binding conditions in combination with quantitative autoradiography to examine the ontogeny of g-, r-and ~-opioid receptors in the developing rat brain. Membrane binding data indicate that the affinities of#-, r-and 6sites for radiolabeled drugs are similar in neonatal and adult rats. g-And r-receptors are present in significant densities during early neonatal periods, while h-receptors appear much later. Autoradiographic data indicate that #-and r-receptors appear early in the development of several brain regions, including the neostriatum, olfactory tubercle and rostral midbrain, and later in other regions such as the thalamus and hypothalamus. Whereas the densities of r-binding sites remain relatively constant throughout development, there is a transient appearance and/or redistribution of#-receptors in several brain areas. &Receptors are present in low densities in the basal forebrain at birth. The level of h-receptor binding increases markedly during the third postnatal week in all brain areas examined. The early appearance of#-and r-receptors during the ontogeny of the brain suggests that these receptors, at least in part, mediate the developmental actions of exogenous and endogenous opioids.