• thereby, inhibiting the agonist effects of prolactin on prolactin receptors. (wikipedia.org)
  • Semisynthetic ergot alkaloid derivative with strong dopamine D2-receptor agonist and partial dopamine D1-receptor effects. (medscape.com)
  • The present study determined whether the serotonin2A (5-HT2A) receptors in the hypothalamic paraventricular nucleus mediate the neuroendocrine responses to a peripheral injection of the 5-HT2A/2Creceptor agonist (−)DOI [(−)1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane]. (ku.edu)
  • Mesulergine hydrochloride is a 5-HT 2A and 2C receptor antagonist (pA 2 values are 9.1 for each receptor) and D 2 -like dopamine receptor partial agonist (K i = 8 nM). (tocris.com)
  • DOSTINEX Tablets contain cabergoline, a dopamine receptor agonist. (drugs.com)
  • Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D 2 receptors. (drugs.com)
  • After transsphenoidal surgery, these agents are generally a first-line treatment, followed by a dopamine-receptor agonist or GH receptor antagonist. (medscape.com)
  • This is the dopamine-receptor agonist that is most often used to treat GH and prolactin excess. (medscape.com)
  • Cabergoline is a potent dopamine-receptor agonist with a prolonged duration of action. (medscape.com)
  • The anterior pituitary hormone prolactin is present in the circulation in both males and females, with widespread expression of the prolactin receptor throughout the forebrain. (nih.gov)
  • They act on postsynaptic dopamine receptors while causing no effect on other anterior pituitary functions. (medscape.com)
  • The preparation, identification and assay of prolactin - a hormone of the anterior pituitary. (scielo.br)
  • The secretion of prolactin by the anterior pituitary is mainly under hypothalamic inhibitory control, likely exerted through release of dopamine by tuberoinfundibular neurons. (drugs.com)
  • The prolactin receptor (PRLR) is a membrane-bound protein of the cytokine receptor superfamily. (wikipedia.org)
  • Regulation of metabolic homeostasis by the TGF-beta superfamily receptor ALK7. (nih.gov)
  • Cabergoline decreased serum prolactin levels in reserpinized rats. (drugs.com)
  • cabergoline n=168), DOSTINEX produced a dose-related decrease in serum prolactin levels with prolactin normalized after 4 weeks of treatment in 29%, 76%, 74% and 95% of the patients receiving 0.125, 0.5, 0.75, and 1.0 mg twice weekly respectively. (drugs.com)
  • Relation between serum prolactin levels and antipsychotic response to risperidone in patients with schizophrenia. (cdc.gov)
  • Lanreotide also significantly decreases prostaglandin E1-stimulated jejunal secretion of water, sodium, potassium, and chloride and reduces prolactin levels in acromegalic patients undergoing long-term treatment. (medscape.com)
  • Recognizes the ligand binding site of rat prolactin receptor. (enzolifesciences.com)
  • Another method of inhibit surface area receptor signaling has been antireceptor antibodies that stop either ligand binding or receptor activation (30, 31). (imacst.com)
  • Here we show that the in vivo administration of MPA triggers massive induction of the key osteoclast differentiation factor RANKL (receptor activator of NF-κB ligand) in mammary-gland epithelial cells. (nature.com)
  • Upon ligand binding, type I receptors phosphorylate cytoplasmic SMAD transcription factors, which then translocate to the nucleus and interact directly with DNA or in complex with other transcription factors (Bondestam et al. (nih.gov)
  • How is a receptor-ligand binding curve determined? (flashcardmachine.com)
  • Describe the three lines on a receptor-ligand binding curve? (flashcardmachine.com)
  • Fast receptor systems, such as the GABAA receptor and the nicotinic receptor at the neuromuscular junction, involve the direct binding of a neurotransmitter to a ligand-gated channel, which opens or closes the channel. (psychiatrictimes.com)
  • Circulating osteoprotegerin (OPG), a member of the receptor activator of nuclear factor kappa-B (RANK) axis, may influence breast cancer risk via its role as the decoy receptor for both the RANK ligand (RANKL) and tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). (biomedcentral.com)
  • Bone homeostasis is maintained by the interplay between the receptor activator of nuclear factor kappa-B (RANK), its soluble activation ligand (RANKL), and OPG. (biomedcentral.com)
  • This study observed reduced breast cancer risk among women with comparatively high OPG concentrations, but given a small number of incident cases ( n = 76), risk by tumor subtypes (e.g., by estrogen (ER) and progesterone (PR) receptor status) was not investigated. (biomedcentral.com)
  • The most extensively studied and used somatostatin analogue, octreotide, binds to the somatostatin receptor subtypes II and V, inhibiting GH secretion. (medscape.com)
  • Octreotide acts primarily on somatostatin receptor subtypes II and V, inhibiting GH secretion. (medscape.com)
  • Discovery and characterization of prolactin neutralizing monoclonal antibodies for the treatment of female-prevalent pain disorders. (iasp-pain.org)
  • When a neurotransmitter binds to a receptor, an extracellular signal is transduced into an intracellular one, causing a functional change inside target neurons. (psychiatrictimes.com)
  • OPG binds RANKL as a decoy receptor, inhibiting the activation of RANK by RANKL and preventing the differentiation of bone marrow precursor (monocyte/macrophage) cells to osteoclasts - cells that are central in the process of bone resorption [ 2 ]. (biomedcentral.com)
  • Pasireotide is a cyclohexapeptide somatostatin analog that binds to human somatostatin receptors 1, 2, 3, 4 and 5. (medscape.com)
  • It selectively binds to GH receptors on cell surfaces, blocking endogenous GH binding. (medscape.com)
  • GH-dependent signaling is usually activated by GHR's adoption of the dimerized construction that activates the receptor-associated cytoplasmic tyrosine kinase, Janus kinase 2 (JAK2), and additional kinases and following engagement from the sign transducer and activator of transcription (STAT), sTAT5A/B particularly, ERK, phosphatidylinositol-3 kinase, and additional pathways (18C25). (imacst.com)
  • What are physical characteristics found in all tyrosine kinase receptors? (flashcardmachine.com)
  • How is the insulin tyrosine kinase receptor unusual? (flashcardmachine.com)
  • How is a tyrosine kinase receptor activated? (flashcardmachine.com)
  • Coexpression and cross-regulation of the prolactin receptor and sex steroid hormone receptors in breast cancer. (qxmd.com)
  • The basis for this hormonal synergy is unknown, but may involve cellular coexpression of the sex steroid and PRL receptors, coupled with receptor cross-regulation. (qxmd.com)
  • Regulation of sex steroid receptors by PRL and of the PRL receptor by sex steroids was examined in T-47D and MCF-7 breast cancer cells. (qxmd.com)
  • We subsequently investigated changes in the negative-feedback regulation of prolactin secretion and prolactin-induced suppression of luteinising hormone (LH) pulsatile secretion in aged male mice. (nih.gov)
  • Feedback regulation of prolactin secretion appeared to be unaffected in aged males, with no change in levels of circulating prolactin, and normal prolactin-induced phosphorylated signal transducer and activator of transcription 5(pSTAT5) immunoreactivity in tuberoinfundibular dopaminergic (TIDA) neurones in the arcuate nucleus. (nih.gov)
  • There is growing evidence that TNF-alpha and its two receptors play an important role in hormonal regulation, metabolism, inflammation and cancer. (aaem.pl)
  • all of these hormones' regulation is believed controlled, to some extent, by serotonin receptors in the brain. (erowid.org)
  • While prior publications have addressed the presence of sexual dysfunction (SD) among men with PD, there has been a paucity of work examining the hypothalamic-pituitary-gonadal (HPG) axis and the interplay between dopamine, prolactin (PRL), and testosterone. (nature.com)
  • Furthermore, while some research suggests that PD patients are at higher risk for prolactin elevation and testosterone deficiency, heterogeneity of the data limits extrapolation. (nature.com)
  • Distinct roles of the two tumor necrosis factor (TNF) receptors in modulating TNF and lymphotoxin alpha effects. (aaem.pl)
  • Engelmann H, Holtmann H, Brakebusch C, Avni YS, Sarov I, Nophar Y, Hadas E, Leitner O, Wallach D. Antibodies to a soluble form of a tumor necrosis factor (TNF) receptor have TNF-like activity. (aaem.pl)
  • Aderka D, Engelmann H, Maor Y, Brakebusch C, Wallach D. Stabilization of the bioactivity of tumor necrosis factor by its soluble receptors. (aaem.pl)
  • Chegini N. An inverse relation between the expression of tumor necrosis factor alpha (TNF-alpha) and TNF-alpha receptor in human endometrium. (aaem.pl)
  • Onsrud M, Shabana A, Austgulen R, Nustad K. Comparison between soluble tumor necrosis factor receptors and CA125 in peritoneal fluids as a marker for epithelial ovarian cancer. (aaem.pl)
  • Genetic inactivation of the RANKL receptor RANK in mammary-gland epithelial cells prevents MPA-induced epithelial proliferation, impairs expansion of the CD49f hi stem-cell-enriched population, and sensitizes these cells to DNA-damage-induced cell death. (nature.com)
  • Stat 5a Knockout: Stat5a deficiency results in the loss of prolactin-dependent mammary gland development and lactogenesis. (nih.gov)
  • Prolactin induces mammary gland development and lactogenesis. (nih.gov)
  • The PRLR is a class 1 cytokine receptor that uses messenger pathways to control cell proliferation, migration, intracellular ion concentration and inhibit programmed cell death (apoptosis). (wikipedia.org)
  • In this area, dopamine acts directly to inhibit the release of prolactin. (psychiatrictimes.com)
  • The prolactin-lowering efficacy of DOSTINEX was demonstrated in hyperprolactinemic women in two randomized, double-blind, comparative studies, one with placebo and the other with bromocriptine. (drugs.com)
  • bromocriptine n=236 in the intent-to-treat analysis), prolactin was normalized in 77% of the patients treated with DOSTINEX at 0.5 mg twice weekly compared with 59% of those treated with bromocriptine at 2.5 mg twice daily. (drugs.com)
  • It inhibits prolactin secretion more effectively than bromocriptine. (medscape.com)
  • Concomitant activation of the insulin-like growth factor-1 receptor, Akt, and extracellular signal-regulated protein kinase 1 and 2 as well as increased phosphorylation of Bad also were unique to the hippocampus of APP Sw mice. (jneurosci.org)
  • It is suggested that dopamine exerts an inhibitory control over prolactin release from the adenohypophysis by inhibiting the release of prolactin-inhibiting factor (PIF) from the median eminence and by acting directly on the pituitary to suppress prolactin release. (elsevierpure.com)
  • Defects on prolactin receptor signalling can trigger tumour activity, rather than suppress. (wikipedia.org)
  • There were, however, significant impairments in the ability of prolactin to suppress LH pulsatile secretion in aged males. (nih.gov)
  • In contrast, prolactin did not suppress LH pulse frequency in aged males, with prolactin leading to an increase in mean LH concentration. (nih.gov)
  • Investigations in two IGSF1 knockout mouse models converged to show that IGSF1 deficiency leads to reduced expression of the receptor for thyrotropin-releasing hormone (TRH) and impaired TRH stimulation of thyrotropin secretion, providing a candidate mechanism for the central hypothyroidism observed in patients. (medscape.com)
  • The prolactin receptor (PRLR) is a type I cytokine receptor encoded in humans by the PRLR gene on chromosome 5p13-14. (wikipedia.org)
  • Neither the 5-HT2A receptor antagonist nor the 5-HT2Creceptor antagonist, injected alone, altered the basal levels of these hormones. (ku.edu)
  • Estrogens are steroid hormones that act through their receptors (ER) α and β. (intechopen.com)
  • Analysis of sex steroid receptor messenger ribonucleic acid and binding activity showed that acute PRL treatment produced a time- and concentration-dependent increase in progesterone receptor and a decrease in androgen receptor. (qxmd.com)
  • GH-receptor agonists are the newest class of drugs used to decrease excessive GH effect. (medscape.com)
  • We also found that SRC-3 depletion in cultured HESCs results in a significant attenuation in the induction of a wide-range of established biomarkers of decidualization, despite exposure of these cells to a deciduogenic stimulus and normal progesterone receptor expression. (frontiersin.org)
  • Ojeda, SR, Harms, PG & McCann, SM 1974, ' Effect of Blockade of Dopaminergic Receptors on Prolactin and LH Release: Median Eminence and Pituitary Sites of Action ', Endocrinology , vol. 94, no. 6, pp. 1650-1657. (elsevierpure.com)
  • In 1963, Carlsson first postulated that the effects of neuroleptics were secondary to dopamine receptor blockade. (psychiatrictimes.com)
  • Genetic associations of prolactin increase in olanzapine/fluoxetine combination-treated patients. (cdc.gov)
  • Prolactin (PRL) has recently been demonstrated to elicit female-selective nociceptor sensitization and increase pain-like behaviors in female animals. (iasp-pain.org)
  • Clomiphene citrate was first released for use in 1967 and is in the category of drugs known as SERMs (selective estrogen receptor modulators). (pacificfertility.ca)
  • Cabergoline is in a class of medications called dopamine receptor agonists. (medlineplus.gov)
  • Receptor-binding studies indicate that cabergoline has low affinity for dopamine D 1 , α 1 - and α 2 -adrenergic, and 5-HT 1 - and 5-HT 2 -serotonin receptors. (drugs.com)
  • The prolonged prolactin-lowering effect of cabergoline may be related to its slow elimination and long half-life. (drugs.com)
  • Dorsomedial hypothalamic nucleus: lipidized prolactin-releasing peptide increases neuronal activity in dorsomedial hypothalamic nucleus and induces c-fos and FosB expression in neurons. (guidetopharmacology.org)
  • Anatomical profiling of G protein-coupled receptor expression. (guidetopharmacology.org)
  • To examine this hypothesis the expression of the sex steroid and PRL receptors was examined in 20 human breast cancer cell lines and 123 primary breast cancers. (qxmd.com)
  • The level of PRL receptor expression in the breast cancer cell lines was linearly related to that of the estrogen and progesterone receptors, but not to that of the androgen receptor. (qxmd.com)
  • ALK7 expression in prolactinoma is associated with reduced prolactin and increased proliferation. (nih.gov)
  • Decreased expression of activin A receptor 1C may result in Ca(2+) -induced aberrant skin hypersensitivity. (nih.gov)
  • Correction: Expression of hormone receptors is associated with specific immunological profiles of the breast cancer microenvironment. (medscape.com)
  • In this organ, estrogens promote or limit cell proliferation depending on the activated receptor, with implications for the pathophysiology of benign prostatic hyperplasia (BPH) and prostate cancer (PCa). (intechopen.com)
  • Moreover, IGSF1 mutations are also commonly associated with other clinical phenotypes, including prolactin and growth hormone dysregulation, and macroorchidism. (medscape.com)
  • abstract = "Pimozide, a dopamine receptor blocker, was injected SC or implanted into the hypothalamus or adenohypophysis of ovariectomized rats to determine its effect on the release of LH and prolactin. (elsevierpure.com)
  • Recent advances in molecular genetics have revealed the two-receptor model to be a gross oversimplification. (psychiatrictimes.com)
  • Molecular Biology of the Channel Catfish Gonadotropin Receptors: 2. (biolreprod.org)
  • Olsson I, Gatanaga T, Gullberg U, Lantz M, Granger GA. Tumour necrosis factor (TNF) binding proteins (soluble TNF receptor forms) with possible roles in inflammation and malignancy. (aaem.pl)
  • Opala T, Rzymski P, Wilczak M, Woźniak J. Evaluation of soluble tumour necrosis factor alpha receptors p55 and p75 in ovarian cancer patients. (aaem.pl)
  • SCR-6852, an oral and highly brain-penetrating estrogen receptor degrader (SERD), effectively shrinks tumors both in intracranial and subcutaneous ER + breast cancer models. (medscape.com)
  • In MCF-7 and T-47D cells, acute treatment with progestins and androgens and long term treatment with estrogens increased PRL receptor levels. (qxmd.com)
  • We aimed to investigate prolactin transport into the brain, as well as circulating levels of prolactin and functional responses to prolactin, in aged male mice (23 months). (nih.gov)
  • Prolactin is an important hormone involved in the interaction between maternal, extraembryonic, and fetal tissues that remains in high levels during the entire duration of pregnancy . (bvsalud.org)
  • Prolactin levels are often adequately suppressed with dopamine-receptor agonists. (medscape.com)
  • The effect of the Taq1A variant in the dopamine D2 receptor gene and common CYP2D6 alleles on prolactin levels in risperidone-treated boys. (cdc.gov)
  • Variants in the DRD2 locus and antipsychotic-related prolactin levels: A meta-analysis. (cdc.gov)
  • Dopamine-receptor agonists make up another pharmacologic option. (medscape.com)
  • Lanreotide elicits high affinity for human somatostatin receptors 2, 3, and 5. (medscape.com)
  • A serotonin-containing nerve cell which is stimulated beyond a certain threshold 'fires,' releasing serotonin into the synapse, which then attaches to specialized sites on the 'receiving' nerve cell called 'receptors. (erowid.org)
  • Serotonin attaches to its receptors, thus modifying the electrical activity of the receiving cell, which in turn either fires itself, or is prevented from firing. (erowid.org)
  • Thus, we are interesting in determine which serotonin receptors, in man, mediate specific effects of DMT. (erowid.org)
  • Now that we have this data describing effects of DMT by itself, we can pre-treat subjects with drugs that block certain types of serotonin receptors, and see what happens to these factors. (erowid.org)
  • For example, if pre-treatment with a serotonin-1A blocking drug enhances visual effects, but reduces beta-endorphin stimulation, we can suggest that the serotonin-1A receptor mediates those functions. (erowid.org)
  • International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). (tocris.com)
  • Although LFA102 has been proved sufficient to reduce prolactin receptor signaling based on in vitro and in vivo (mouse) studies, LFA102 likely has low effects on limiting tumor growth (breast and prostate cancer) as shown in phase I clinical trials. (wikipedia.org)
  • These results indicate that receptors for sex steroids and PRL are coexpressed and are cross-regulated, providing a potential mechanism for the observed synergy among estrogen, progesterone, and PRL in the control of tumor growth. (qxmd.com)
  • Effect of prolactin and growth hormone on prolactin and lh receptors in the dwarf mouse. (jax.org)
  • LFA102 is a monoclonal antibody that has been studied and tested for disrupting prolactin receptor's signaling in breast cancers and prostate cancers. (wikipedia.org)