Molecular neurobiology and pharmacology of the Vasopressin/Oxytocin receptor family

Peter, J.; Burbach, Harold J.; Adan, Roger A.H.; Lolait, Stephen J.; Leeuwen, Fred W. van; Mezey, Éva; Palkovits, Miklós; Barberis, Claude

doi:10.1007/bf02071318

Cited by 106 publications

(47 citation statements)

References 78 publications

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“…Since OT/vasopressin analogues bind to and activate four different receptor subtypes (OTR, V1a, V1b and V2) (Chini et al, 1995b;Peter et al, 1995;Barberis et al, 1999), peptides of potential clinical use should be checked for their receptor selectivity. Our competition experiments on receptor-rich membrane preparations showed that dLVT binds to human OTR, V1a, V1b and V2 with a pharmacological profile that is very similar to that of OT.…”

Section: Discussionmentioning

confidence: 99%

“…OT/AVP analogues bind to and activate (albeit with different affinities and efficacies) all members of the OT/AVP receptor family, which includes the OTR and the three vasopressin receptor subtypes V1a, V1b and V2 (Peter et al, 1995;Chini et al, 1995b;Barberis et al, 1999). When developing a specific OTR analogue, it is therefore essential to check its binding properties not only on the human OTR, but also on the V1a, V1b and V2 subtypes.…”

Section: Receptor Selectivitymentioning

confidence: 99%

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Improved radiotracing of oxytocin receptor-expressing tumours using the new [111In]-DOTA-Lys8-deamino-vasotocin analogue

et al. 2003

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Oxytocin receptors (OTR) have been described in a number of tumours of different origin, and represent a new target for specific radiolabelled oxytocin (OT) analogues in cancer diagnosis and therapy. By linking the DOTA chelating agent to position 8 of the deamino derivative of Lys 8 -vasotocin (dLVT), we obtained a new compound (DOTA-dLVT) with the following characteristics: (1) it forms a monomeric and stable compound that binds to OTR with an affinity comparable to that of the endogenous OT ligand; (2) it is characterised by a very good selectivity profile for the human OTR, with a low affinity binding to the closely related V1a, V1b and V2 vasopressin receptor subtypes; (3) it induces rapid and persistent receptor internalisation and (4) when radiolabelled, [ 111 In]-DOTA-dLVT is efficiently and selectively taken up by OTR-positive tumours grown in mice. These features makes radiolabelled DOTA-dLVT a very good candidate for the radiotargeting of OTR-expressing tumours.

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Section: Discussionmentioning

confidence: 99%

Section: Receptor Selectivitymentioning

confidence: 99%

Improved radiotracing of oxytocin receptor-expressing tumours using the new [111In]-DOTA-Lys8-deamino-vasotocin analogue

et al. 2003

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“…However, the previous studies revealed that magnocellular VP could act as secretagogues for ACTH as well, reaching the anterior pituitary via several vascular pathways [15]. It was shown that VP binds to three G protein-coupled receptors, among which V1b receptors are primarily located at the corticotroph surface regulating ACTH secretion [16][17][18][19][20][21]. Although the role of VP in chronic stress response is well documented, it is still unclear how acute exposure to different types of stressors affects VP influence on ACTH secretion [22].…”

Section: Introductionmentioning

confidence: 99%

The effect of acute heat exposure on rat pituitary corticotroph activation: the role of vasopressin.

Jasnić

Korać²,

Veličković³

et al. 2011

Folia Histochem Cytobiol.

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Abstract:The increased ambient temperature affects the function of hypothalamic-pituitary-adrenal (HPA) axis. Since the correlation among vasopressin (VP), adrenocorticotropic hormone (ACTH) and corticosterone (CORT) responses to various stressors have been long recognized, the aim of this study was to reveal the aforementioned hormones production and morphology of the pituitary gland after exposure to acute heat. Rats were exposed to high ambient temperature (38°C) for 20 or 60 minutes. The circulating hormones were determined by an ELISA test or chemiluminescence's method. The results obtained show the elevation in ACTH and CORT secretion depending on the duration of heat exposure. The VP concentration increased only after prolonged exposure to heat (60 min). The pituitary morphology was examined by routine and fluorescent immunohistochemistry as well as electron microscopy. Observed changes in the anterior and posterior pituitary well corresponded to circulating hormones, regarding the volume density of ACTH-immunopositive cells, percentage of ACTH immunopositive area v. total area and number of VP-immunopositive containing varicose fibers per total area. Acute heat exposure also induced changes in shapes of ACTH-immunopositive cells. Cells appeared stellate with numerous slender cytoplasmic processes and degranulated, which is the most obvious after 20 min. In addition, immunopositivity of endothelial and anterior pituitary cells for VP suggests its influence on ACTH secretion.

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“…In addition, VP secreted within the central nervous system (CNS), modulates neuronal function acting as a neurotransmitter. The functions of VP are mediated through membrane VP receptors belonging to the G proteincoupled membrane receptor (GPCR) superfamily (4). There are two major VP receptor subtypes, V1, which is coupled to calcium phospholipid dependent pathways, and V2, which is coupled to cAMP-dependent pathways.…”

Section: Introductionmentioning

confidence: 99%

Anti-apoptotic actions of vasopressin in H32 neurons involve map kinase transactivation and bad phosphorylation

Volpi¹,

Aguilera²

2008

Experimental Neurology

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Vasopressin (VP) secreted within the brain modulates neuronal function acting as a neurotransmitter. Based on the observation that VP prevented serum deprivation-induced cell death in the neuronal cell line, H32, which expresses endogenous V1 receptors, we tested the hypothesis that VP has antiapoptotic properties. Flow cytometry experiments showed that 10nM VP prevented serum deprivation-induced cell death and annexin V binding. Serum deprivation increased caspase-3 activity in a time and serum concentration dependent manner, and VP prevented these effects through interaction with receptors of V1 subtype. The signaling pathways mediating the anti-apoptotic effect of VP involve mitogen activated protein (MAP) kinase and extracellular signal-regulated kinases (ERK), Ca 2+ /calmodulin dependent kinase (CaMK) and protein kinase C (PKC). Western blot analyses revealed time-dependent decreases of Bad phosphorylation and increases in cytosolic levels of cytochrome c following serum deprivation, effects which were prevented by 10nM VP. These data demonstrate that activation of endogenous V1 VP receptors prevents serum deprivation-induced apoptosis, through phosphorylation-inactivation of the pro-apoptotic protein, Bad, and consequent decreases in cytosolic cytochome c and caspase-3 activation. The data suggest that VP has antiapoptotic activity in neurons and that VP may act as a neuroprotective agent in the brain.

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Molecular neurobiology and pharmacology of the Vasopressin/Oxytocin receptor family

Cited by 106 publications

References 78 publications

Improved radiotracing of oxytocin receptor-expressing tumours using the new [111In]-DOTA-Lys8-deamino-vasotocin analogue

Improved radiotracing of oxytocin receptor-expressing tumours using the new [111In]-DOTA-Lys8-deamino-vasotocin analogue

The effect of acute heat exposure on rat pituitary corticotroph activation: the role of vasopressin.

Anti-apoptotic actions of vasopressin in H32 neurons involve map kinase transactivation and bad phosphorylation

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