GPR171

GPR171, also known as platelet activating factor H963, is a member of the class A rhodopsin family of heterotrimeric G-protein coupled receptors. Until 2013, GPR171 was an orphan receptor, it is now known to be activated by the endogenous proSAAS-derived peptide BigLEN.

Products
Background
Literature

Agonists

Cat No Product Name / Activity
6304 BigLEN (mouse)
GPR171 agonist
6306 BigLEN (rat)
Potent GPR171 agonist
6299 MS 15203
Potent and selective GPR171 partial agonist

Antagonists

Cat No Product Name / Activity
6298 MS 21570
GPR171 antagonist

GPR171, also known as platelet activating factor H963, is a member of the class A rhodopsin family of heterotrimeric G-protein coupled receptors. Until 2013, GPR171 was an orphan receptor, it is now known to be activated by the endogenous proSAAS-derived peptide BigLEN.

Expressed in the basolateral amygdala, and also in the hypothalamus where it co-localizes with its ligand, BigLEN, GPR171 shows high levels of similarity to P2Y receptors but exhibits different expression patterns and is not activated by carboxylic acids.

Activation of GPR171 has been shown to increase weight gain and food intake in mice, so the receptor is a target for research into obesity and eating disorders. GPR171 is also of interest to cancer researchers, as multiple gene copies are commonly present in cancer cells and are associated with their proliferation and migration. In addition, it has been shown that GPR171 expression inhibits myeloid differentiation in hematopoietic cell lines.

External sources of pharmacological information for GPR171 :

    Literature for GPR171

    Tocris offers the following scientific literature for GPR171 to showcase our products. We invite you to request* or download your copy today!

    *Please note that Tocris will only send literature to established scientific business / institute addresses.


    Cancer

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    GPCR

    GPCR Product Listing

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    Immunology

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    Peptides Involved in Appetite Modulation

    Peptides Involved in Appetite Modulation Scientific Review

    Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

    Stem Cells

    Stem Cells Scientific Review

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    Angiogenesis in Cancer

    Angiogenesis in Cancer Poster

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    Cancer Metabolism

    Cancer Metabolism Poster

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    Epigenetics in Cancer

    Epigenetics in Cancer Poster

    Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

    Gut Hormones

    Gut Hormones Poster

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    Stem Cells

    Stem Cells Poster

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