ArticleBritish journal of pharmacology2006
The basic secretagogue compound 48/80 activates G proteins indirectly via stimulation of phospholipase D-lysophosphatidic acid receptor axis and 5-HT1A receptors in rat brain sections.
Article in British journal of pharmacology, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 58 citations in OpenAlex.
- Anaphylactic Rare Saponins Separated fromEvidence-based complementary and alternative medicine : eCAM · 2022Article
- Tachykinin-1 receptor antagonism suppresses substance-P- and compound 48/80-induced mast cell activation from rat mast cells expressing functional mas-related GPCR B3.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2020Article
- Milonine, an Alkaloid of Cissampelos sympodialis Eichl. (Menispermaceae) Inhibits Histamine Release of Activated Mast Cells.Inflammation · 2017Article
- Inhibitory effect of a new orally active cedrol-loaded nanostructured lipid carrier on compound 48/80-induced mast cell degranulation and anaphylactic shock in mice.International journal of nanomedicine · 2017Article
- Proteomics Study on Nonallergic Hypersensitivity Induced by Compound 4880 and Ovalbumin.PloS one · 2016Article
- Anatomical location of LPA1 activation and LPA phospholipid precursors in rodent and human brain.Journal of neurochemistry · 2015Article
- Autocrine hemokinin-1 functions as an endogenous adjuvant for IgE-mediated mast cell inflammatory responses.The Journal of allergy and clinical immunology · 2015Article
- Eosinophils and mast cells in leishmaniasis.Immunologic research · 2014Review
- Mast cells play no role in the pathogenesis of postoperative ileus induced by intestinal manipulation.PloS one · 2014Article
- Mast cells in the pathogenesis of multiple sclerosis and experimental autoimmune encephalomyelitis.International journal of molecular sciences · 2012Review
- Mast cell degranulation mediates compound 48/80-induced hyperalgesia in mice.Biochemical and biophysical research communications · 2012Article
- Lipid phosphate phosphatase inhibitors locally amplify lysophosphatidic acid LPA1 receptor signalling in rat brain cryosections without affecting global LPA degradation.BMC pharmacology · 2012Article
- Article
- Non-FcεR bearing mast cells secrete sufficient interleukin-4 to control Francisella tularensis replication within macrophages.Cytokine · 2011Article
- Inhibitory effects of curcumin on passive cutaneous anaphylactoid response and compound 48/80-induced mast cell activation.Anatomy & cell biology · 2010Article
- ATX-LPA receptor axis in inflammation and cancer.Cell cycle (Georgetown, Tex.) · 2009Review
- Phospholipase D signaling in serotonin-induced mitogenesis of pulmonary artery smooth muscle cells.American journal of physiology. Lung cellular and molecular physiology · 2008Article
- Article
- Codeine induces human mast cell chemokine and cytokine production: involvement of G-protein activation.Allergy · 2007Article
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The basic secretagogues, such as compound 48/80 (c48/80) and mastoparans, are widely used histamine-releasing agents and their mechanism of action is commonly attributed to a direct, receptor-bypassing property to activate the G(i/o) class of G proteins. We tested here whether c48/80 could directly stimulate [(35)S]guanosine-5'-[gamma-thio]triphosphate ([(35)S]GTPgammaS) binding to rat brain sections in an attempt to visualize the entire signaling pool of G(i/o) in its native neuroanatomical context. Instead of direct G(i/o) activation, c48/80 (100 microg ml(-1)) from various suppliers stimulated brain phospholipase D (PLD) activity, leading to the generation of endogenous phospholipids capable of activating brain white matter-enriched, G(i/o)-coupled lysophosphatidic acid (LPA) receptors. This response was sensitive to 1-butanol and was potently reversed by the LPA(1)/LPA(3) receptor-selective antagonist Ki16425 (IC(50) 59+/-13 nM, mean+/-s.e.m.), and showed age-dependent decline, closely reflecting known developmental regulation of the PLD-LPA(1) receptor axis in the CNS. In addition, c48/80 was found to modestly activate hippocampal 5-HT(1A) receptors in a pH-dependent and antagonist-sensitive manner. Consistent with the lack of direct G(i/o)-activating properties in brain sections, c48/80 showed no activity in classical membrane [(35)S]GTPgammaS binding assays. Instead, c48/80 from one particular manufacturer elicited non-specific effect in these assays, therefore challenging the previous interpretations regarding the compound's ability to activate G proteins directly. We conclude that c48/80 is not a receptor-bypassing general G protein activator but rather activates PLD, leading to generation of endogenous LPA receptor-activating phospholipids. This property may also contribute to the compound's ability to release histamine from mast cells.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.