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gpr52 agonist ftbmt  (Takeda)

 
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    Takeda gpr52 agonist ftbmt
    <t> GPR52 </t> inverse agonists potency.
    Gpr52 Agonist Ftbmt, supplied by Takeda, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/product/ftbmt/tak+041/pmc08219759-16-6-0
    Average 90 stars, based on 1 article reviews
    gpr52 agonist ftbmt - by Bioz Stars, 2026-09
    90/100 stars

    Images

    1) Product Images from "Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918"

    Article Title: Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918

    Journal: Heliyon

    doi: 10.1016/j.heliyon.2021.e07201

    GPR52 inverse agonists potency.
    Figure Legend Snippet: GPR52 inverse agonists potency.

    Techniques Used:

    Literature GPR52 agonists and inverse agonists.
    Figure Legend Snippet: Literature GPR52 agonists and inverse agonists.

    Techniques Used:

    In vitro characterisation of CBD, O-1918 and related compounds. A. CBD, O-1918 and related compounds are inverse agonists in CHO-GPR52 cells when tested alone, reducing cAMP down to the level of CHO-WT (black bar). Basal (DMSO) response from CHO-GPR52 (grey bar) is also shown for comparison, with dotted lines to indicate response level. Data are pooled (mean ± SD) from 4 independent experiments performed in duplicate, normalised to 1 μM 7m response. B. All inverse agonists inhibit an EC 50 concentration of the agonist compound 7m, reducing cAMP levels below the basal level in line with the apparent inverse agonism in A. C. All test compounds are inactive in CHO-WT cells, except for cannabidiol, which shows a small decrease in cellular cAMP beyond the standard deviation of the DMSO response (indicated by dotted lines). Data are pooled (mean ± SD) from 4 independent experiments performed in singlicate expressed as a percentage of the DMSO response.
    Figure Legend Snippet: In vitro characterisation of CBD, O-1918 and related compounds. A. CBD, O-1918 and related compounds are inverse agonists in CHO-GPR52 cells when tested alone, reducing cAMP down to the level of CHO-WT (black bar). Basal (DMSO) response from CHO-GPR52 (grey bar) is also shown for comparison, with dotted lines to indicate response level. Data are pooled (mean ± SD) from 4 independent experiments performed in duplicate, normalised to 1 μM 7m response. B. All inverse agonists inhibit an EC 50 concentration of the agonist compound 7m, reducing cAMP levels below the basal level in line with the apparent inverse agonism in A. C. All test compounds are inactive in CHO-WT cells, except for cannabidiol, which shows a small decrease in cellular cAMP beyond the standard deviation of the DMSO response (indicated by dotted lines). Data are pooled (mean ± SD) from 4 independent experiments performed in singlicate expressed as a percentage of the DMSO response.

    Techniques Used: In Vitro, Comparison, Concentration Assay, Standard Deviation

    Proposed binding modes for CBD and O-1918. A: Crystal structure of c17 (magenta) bound to GPR52, PDB code 6LI0 , water bridge between D188 ECL2 and S299 7.35 in sticks. This structure has been used for the docking experiments. Panel A is left in magenta shade to differentiate it from docking poses in grey. B: Docked pose of CBD (pale yellow) in GPR52 (grey), hydrogen bond with Asp188 ECL2 in dotted lines. C: Overlay of the proposed CBD (pale yellow) binding mode with the binding conformation of c17 from the GRP52 crystal structure (magenta). D: O-1918 (cyan) bound to GPR52 (grey) resembling the proposed CBD binding mode at B. E: O-1918 (green) bound to GPR52 (grey) with an alternate binding mode. F: O-1918 overlay of both proposed binding modes for O-1918, despite its distinct shape the molecule can bind in an almost symmetrical manner.
    Figure Legend Snippet: Proposed binding modes for CBD and O-1918. A: Crystal structure of c17 (magenta) bound to GPR52, PDB code 6LI0 , water bridge between D188 ECL2 and S299 7.35 in sticks. This structure has been used for the docking experiments. Panel A is left in magenta shade to differentiate it from docking poses in grey. B: Docked pose of CBD (pale yellow) in GPR52 (grey), hydrogen bond with Asp188 ECL2 in dotted lines. C: Overlay of the proposed CBD (pale yellow) binding mode with the binding conformation of c17 from the GRP52 crystal structure (magenta). D: O-1918 (cyan) bound to GPR52 (grey) resembling the proposed CBD binding mode at B. E: O-1918 (green) bound to GPR52 (grey) with an alternate binding mode. F: O-1918 overlay of both proposed binding modes for O-1918, despite its distinct shape the molecule can bind in an almost symmetrical manner.

    Techniques Used: Binding Assay

    Related Articles

    Drug discovery:

    Article Title: FTBMT, a Novel and Selective GPR52 Agonist, Demonstrates Antipsychotic-Like and Procognitive Effects in Rodents, Revealing a Potential Therapeutic Agent for Schizophrenia.
    Article Snippet: .. [テキストを入力] [テキストを入力] JPET#242925 1 Title: FTBMT, a novel and selective GPR52 agonist, demonstrates antipsychotic-like and procognitive effects in rodents revealing a potential therapeutic agent for schizophrenia Authors: Keiji Nishiyama , Hirobumi Suzuki, Toshiya Harasawa, Noriko Suzuki, Emi Kurimoto, Takanori Kawai, Minoru Maruyama, Hidetoshi, Komatsu, Kensuke Sakuma, Yuji Shimizu, Masato Shimojo CNS Drug Discovery Unit, Research, Takeda Pharmaceutical Company Limited, Fujisawa, Japan .. KN, HS, TH, NS, EK, TK, MM, HK, YS and MS: CNS Drug Discovery Unit, Research, Takeda Pharmaceutical Company Limited, Fujisawa, Japan KS: Regenerative Medicine Unit, Takeda Pharmaceutical Company Limited, Fujisawa, Japan.

    Article Title: FTBMT, a Novel and Selective GPR52 Agonist, Demonstrates Antipsychotic-Like and Procognitive Effects in Rodents, Revealing a Potential Therapeutic Agent for Schizophrenia.
    Article Snippet: .. Published on August 29, 2017 as DOI: 10.1124/jpet.117.242925 at A SPE T Journals on A ugust 31, 2017 jpet.aspetjournals.org [テキストを入力] [テキストを入力] JPET#242925 2 Running title: FTBMT, a novel GPR52 agonist Corresponding author: Masato Shimojo, Ph.D. CNS Drug Discovery Unit Research Takeda Pharmaceutical Company Ltd. 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan E-mail: masato.shimojo@takeda.com Tel: +81-466-32-1902 Fax: +81-466-29-4543 Number of text pages: 39 Number of tables: 4 Number of figures: 7 Number of references: 54 Number of words in the Abstract: 217 Number of words in the Introduction: 715 Number of words in the Discussion: 1133 Nonstandard abbreviations used: FTBMT: 4-(3-(3-fluoro-5-(trifluoromethyl)benzyl)-5-methyl-1H-1,2,4-triazol-1-yl)-2-methylbenzam ide Recommended section assignment: Neuropharmacology This article has not been copyedited and formatted ..

    Synthesized:

    Article Title: FTBMT, a Novel and Selective GPR52 Agonist, Demonstrates Antipsychotic-Like and Procognitive Effects in Rodents, Revealing a Potential Therapeutic Agent for Schizophrenia.
    Article Snippet: The care and use of the animals and the experimental protocols were approved by the Experimental Animal Care and Use Committee of Takeda Pharmaceutical Company Limited adhered to Act on Welfare and Management of Animals, a Japanese law (Amendment Act No. 46 of 2014). .. FTBMT (Tokumaru et al, 2017) (Figure 1a), was synthesized at Takeda Pharmaceutical Company Limited (Osaka, Japan). .. Olanzapine was extracted from Zyprexa (Eli Lilly and Company, Indianapolis, IN) at KNC Laboratories Co. Ltd. (Kobe, Japan).



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    Image Search Results


    GPR52 inverse agonists potency.

    Journal: Heliyon

    Article Title: Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918

    doi: 10.1016/j.heliyon.2021.e07201

    Figure Lengend Snippet: GPR52 inverse agonists potency.

    Article Snippet: Takeda reported the first example of GPR52 agonists [ ], exemplified by Compound 7m , and subsequently reported related examples such as such as Compound [ ] and the orally bioavailable agonist FTBMT [ ], the pharmacology of which has been extensively characterised in vitro and in vivo.

    Techniques:

    Literature GPR52 agonists and inverse agonists.

    Journal: Heliyon

    Article Title: Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918

    doi: 10.1016/j.heliyon.2021.e07201

    Figure Lengend Snippet: Literature GPR52 agonists and inverse agonists.

    Article Snippet: Takeda reported the first example of GPR52 agonists [ ], exemplified by Compound 7m , and subsequently reported related examples such as such as Compound [ ] and the orally bioavailable agonist FTBMT [ ], the pharmacology of which has been extensively characterised in vitro and in vivo.

    Techniques:

    In vitro characterisation of CBD, O-1918 and related compounds. A. CBD, O-1918 and related compounds are inverse agonists in CHO-GPR52 cells when tested alone, reducing cAMP down to the level of CHO-WT (black bar). Basal (DMSO) response from CHO-GPR52 (grey bar) is also shown for comparison, with dotted lines to indicate response level. Data are pooled (mean ± SD) from 4 independent experiments performed in duplicate, normalised to 1 μM 7m response. B. All inverse agonists inhibit an EC 50 concentration of the agonist compound 7m, reducing cAMP levels below the basal level in line with the apparent inverse agonism in A. C. All test compounds are inactive in CHO-WT cells, except for cannabidiol, which shows a small decrease in cellular cAMP beyond the standard deviation of the DMSO response (indicated by dotted lines). Data are pooled (mean ± SD) from 4 independent experiments performed in singlicate expressed as a percentage of the DMSO response.

    Journal: Heliyon

    Article Title: Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918

    doi: 10.1016/j.heliyon.2021.e07201

    Figure Lengend Snippet: In vitro characterisation of CBD, O-1918 and related compounds. A. CBD, O-1918 and related compounds are inverse agonists in CHO-GPR52 cells when tested alone, reducing cAMP down to the level of CHO-WT (black bar). Basal (DMSO) response from CHO-GPR52 (grey bar) is also shown for comparison, with dotted lines to indicate response level. Data are pooled (mean ± SD) from 4 independent experiments performed in duplicate, normalised to 1 μM 7m response. B. All inverse agonists inhibit an EC 50 concentration of the agonist compound 7m, reducing cAMP levels below the basal level in line with the apparent inverse agonism in A. C. All test compounds are inactive in CHO-WT cells, except for cannabidiol, which shows a small decrease in cellular cAMP beyond the standard deviation of the DMSO response (indicated by dotted lines). Data are pooled (mean ± SD) from 4 independent experiments performed in singlicate expressed as a percentage of the DMSO response.

    Article Snippet: Takeda reported the first example of GPR52 agonists [ ], exemplified by Compound 7m , and subsequently reported related examples such as such as Compound [ ] and the orally bioavailable agonist FTBMT [ ], the pharmacology of which has been extensively characterised in vitro and in vivo.

    Techniques: In Vitro, Comparison, Concentration Assay, Standard Deviation

    Proposed binding modes for CBD and O-1918. A: Crystal structure of c17 (magenta) bound to GPR52, PDB code 6LI0 , water bridge between D188 ECL2 and S299 7.35 in sticks. This structure has been used for the docking experiments. Panel A is left in magenta shade to differentiate it from docking poses in grey. B: Docked pose of CBD (pale yellow) in GPR52 (grey), hydrogen bond with Asp188 ECL2 in dotted lines. C: Overlay of the proposed CBD (pale yellow) binding mode with the binding conformation of c17 from the GRP52 crystal structure (magenta). D: O-1918 (cyan) bound to GPR52 (grey) resembling the proposed CBD binding mode at B. E: O-1918 (green) bound to GPR52 (grey) with an alternate binding mode. F: O-1918 overlay of both proposed binding modes for O-1918, despite its distinct shape the molecule can bind in an almost symmetrical manner.

    Journal: Heliyon

    Article Title: Characterisation of inverse agonism of the orphan-G protein-coupled receptor GPR52 by cannabinoid ligands Cannabidiol and O-1918

    doi: 10.1016/j.heliyon.2021.e07201

    Figure Lengend Snippet: Proposed binding modes for CBD and O-1918. A: Crystal structure of c17 (magenta) bound to GPR52, PDB code 6LI0 , water bridge between D188 ECL2 and S299 7.35 in sticks. This structure has been used for the docking experiments. Panel A is left in magenta shade to differentiate it from docking poses in grey. B: Docked pose of CBD (pale yellow) in GPR52 (grey), hydrogen bond with Asp188 ECL2 in dotted lines. C: Overlay of the proposed CBD (pale yellow) binding mode with the binding conformation of c17 from the GRP52 crystal structure (magenta). D: O-1918 (cyan) bound to GPR52 (grey) resembling the proposed CBD binding mode at B. E: O-1918 (green) bound to GPR52 (grey) with an alternate binding mode. F: O-1918 overlay of both proposed binding modes for O-1918, despite its distinct shape the molecule can bind in an almost symmetrical manner.

    Article Snippet: Takeda reported the first example of GPR52 agonists [ ], exemplified by Compound 7m , and subsequently reported related examples such as such as Compound [ ] and the orally bioavailable agonist FTBMT [ ], the pharmacology of which has been extensively characterised in vitro and in vivo.

    Techniques: Binding Assay