human serotonin 5 ht2a receptor (Revvity)
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human serotonin 5 ht2a receptor
Human Serotonin 5 Ht2a Receptor, supplied by Revvity, used in various techniques. Bioz Stars score: 91/100, based on 18 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/human+serotonin+5+ht2a+receptor/Serotonin+5-HT2A+AequoScreen%3B+cell+line/10__3390_slash_molecules26154605-183-34-38
Average 91 stars, based on 18 article reviews
Human Serotonin 5 Ht2a Receptor, supplied by Revvity, used in various techniques. Bioz Stars score: 91/100, based on 18 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/product/human+serotonin+5+ht2a+receptor/Serotonin+5-HT2A+AequoScreen%3B+cell+line/10__3390_slash_molecules26154605-183-34-38
Average 91 stars, based on 18 article reviews
human serotonin 5 ht2a receptor - by Bioz Stars,
2026-09
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In Vitro:Article Title: Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants Article Snippet: Accepted Manuscript Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants Przemysław Zaręba, Jolanta Jaśkowska, Izabela Czekaj, Grzegorz Satała PII: S0968-0896(19)30783-7 DOI: https://doi.org/10.1016/j.bmc.2019.06.028 Reference: BMC 14965 To appear in: Bioorganic & Medicinal Chemistry Received Date: 9 May 2019 Revised Date: 17 June 2019 Accepted Date: 18 June 2019 Please cite this article as: Zaręba, P., Jaśkowska, J., Czekaj, I., Satała, G., Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants, Bioorganic & Medicinal Chemistry (2019), doi: https://doi.org/10.1016/j.bmc.2019.06.028 This is a PDF file of an unedited manuscript that has been accepted for publication.. As a service to our customers we are providing this early version of the manuscript.. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Article Title: New dual ligands for the D 2 and 5-HT 1A receptors from the group of 1,8-naphthyl derivatives of LCAP. Article Snippet: Accepted Manuscript New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP Przemysław Zaręba, Jolanta Jaśkowska, Paweł Śliwa, Grzegorz Satała PII: S0960-894X(19)30409-3 DOI: https://doi.org/10.1016/j.bmcl.2019.06.029 Reference: BMCL 26507 To appear in: Bioorganic & Medicinal Chemistry Letters Received Date: 7 May 2019 Revised Date: 17 June 2019 Accepted Date: 19 June 2019 Please cite this article as: Zaręba, P., Jaśkowska, J., Śliwa, P., Satała, G., New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP, Bioorganic & Medicinal Chemistry Letters (2019), doi: https://doi.org/10.1016/j.bmcl.2019.06.029 This is a PDF file of an unedited manuscript that has been accepted for publication.. As a service to our customers we are providing this early version of the manuscript.. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Binding Assay:Article Title: Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants Article Snippet: Accepted Manuscript Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants Przemysław Zaręba, Jolanta Jaśkowska, Izabela Czekaj, Grzegorz Satała PII: S0968-0896(19)30783-7 DOI: https://doi.org/10.1016/j.bmc.2019.06.028 Reference: BMC 14965 To appear in: Bioorganic & Medicinal Chemistry Received Date: 9 May 2019 Revised Date: 17 June 2019 Accepted Date: 18 June 2019 Please cite this article as: Zaręba, P., Jaśkowska, J., Czekaj, I., Satała, G., Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants, Bioorganic & Medicinal Chemistry (2019), doi: https://doi.org/10.1016/j.bmc.2019.06.028 This is a PDF file of an unedited manuscript that has been accepted for publication.. As a service to our customers we are providing this early version of the manuscript.. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Article Title: New dual ligands for the D 2 and 5-HT 1A receptors from the group of 1,8-naphthyl derivatives of LCAP. Article Snippet: Accepted Manuscript New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP Przemysław Zaręba, Jolanta Jaśkowska, Paweł Śliwa, Grzegorz Satała PII: S0960-894X(19)30409-3 DOI: https://doi.org/10.1016/j.bmcl.2019.06.029 Reference: BMCL 26507 To appear in: Bioorganic & Medicinal Chemistry Letters Received Date: 7 May 2019 Revised Date: 17 June 2019 Accepted Date: 19 June 2019 Please cite this article as: Zaręba, P., Jaśkowska, J., Śliwa, P., Satała, G., New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP, Bioorganic & Medicinal Chemistry Letters (2019), doi: https://doi.org/10.1016/j.bmcl.2019.06.029 This is a PDF file of an unedited manuscript that has been accepted for publication.. As a service to our customers we are providing this early version of the manuscript.. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Article Title: Dual 5-HT 6 and D 3 Receptor Antagonists in a Group of 1 H -Pyrrolo[3,2- c ]quinolines with Neuroprotective and Procognitive Activity. Article Snippet: .. Cell culture and preparation of cell membranes for radioligand binding assays All the experiments were carried our according to the previously published procedures.32,51,52 HEK293 cells with stable expression of human 5-HT1A, 5-HT2A, 5-HT6, 5- HT7b and D2L receptors (prepared with the use of Lipofectamine 2000) or CHO-K1 cells with plasmid containing the sequence coding for the Cell Culture:Article Title: Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants Article Snippet: Accepted Manuscript Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants Przemysław Zaręba, Jolanta Jaśkowska, Izabela Czekaj, Grzegorz Satała PII: S0968-0896(19)30783-7 DOI: https://doi.org/10.1016/j.bmc.2019.06.028 Reference: BMC 14965 To appear in: Bioorganic & Medicinal Chemistry Received Date: 9 May 2019 Revised Date: 17 June 2019 Accepted Date: 18 June 2019 Please cite this article as: Zaręba, P., Jaśkowska, J., Czekaj, I., Satała, G., Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants, Bioorganic & Medicinal Chemistry (2019), doi: https://doi.org/10.1016/j.bmc.2019.06.028 This is a PDF file of an unedited manuscript that has been accepted for publication.. As a service to our customers we are providing this early version of the manuscript.. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Article Title: New dual ligands for the D 2 and 5-HT 1A receptors from the group of 1,8-naphthyl derivatives of LCAP. Article Snippet: Accepted Manuscript New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP Przemysław Zaręba, Jolanta Jaśkowska, Paweł Śliwa, Grzegorz Satała PII: S0960-894X(19)30409-3 DOI: https://doi.org/10.1016/j.bmcl.2019.06.029 Reference: BMCL 26507 To appear in: Bioorganic & Medicinal Chemistry Letters Received Date: 7 May 2019 Revised Date: 17 June 2019 Accepted Date: 19 June 2019 Please cite this article as: Zaręba, P., Jaśkowska, J., Śliwa, P., Satała, G., New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP, Bioorganic & Medicinal Chemistry Letters (2019), doi: https://doi.org/10.1016/j.bmcl.2019.06.029 This is a PDF file of an unedited manuscript that has been accepted for publication.. As a service to our customers we are providing this early version of the manuscript.. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Article Title: Dual 5-HT 6 and D 3 Receptor Antagonists in a Group of 1 H -Pyrrolo[3,2- c ]quinolines with Neuroprotective and Procognitive Activity. Article Snippet: .. Cell culture and preparation of cell membranes for radioligand binding assays All the experiments were carried our according to the previously published procedures.32,51,52 HEK293 cells with stable expression of human 5-HT1A, 5-HT2A, 5-HT6, 5- HT7b and D2L receptors (prepared with the use of Lipofectamine 2000) or CHO-K1 cells with plasmid containing the sequence coding for the Expressing:Article Title: Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants Article Snippet: Accepted Manuscript Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants Przemysław Zaręba, Jolanta Jaśkowska, Izabela Czekaj, Grzegorz Satała PII: S0968-0896(19)30783-7 DOI: https://doi.org/10.1016/j.bmc.2019.06.028 Reference: BMC 14965 To appear in: Bioorganic & Medicinal Chemistry Received Date: 9 May 2019 Revised Date: 17 June 2019 Accepted Date: 18 June 2019 Please cite this article as: Zaręba, P., Jaśkowska, J., Czekaj, I., Satała, G., Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants, Bioorganic & Medicinal Chemistry (2019), doi: https://doi.org/10.1016/j.bmc.2019.06.028 This is a PDF file of an unedited manuscript that has been accepted for publication.. As a service to our customers we are providing this early version of the manuscript.. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Article Title: N-Skatyltryptamines—Dual 5-HT6R/D2R Ligands with Antipsychotic and Procognitive Potential Article Snippet: .. HEK293 cells (ATCC) with the stable expression of human serotonin 5-HT1AR, 5-HT6, and 5-HT7bR or dopamine D2LR (obtained using of Lipofectamine 2000, Invitrogen) or CHO-K1 cells with plasmid containing the sequence coding for the Article Title: Chlorine substituents and linker topology as factors of 5-HT6R activity for novel highly active 1,3,5-triazine derivatives with procognitive properties in vivo Article Snippet: .. HEK293 cells with stable expression of human 5-HT6, 5-HT7b and D2L receptors (prepared with the use of Lipofectamine 2000) or CHO-K1 cells with plasmid containing the sequence coding for the Article Title: New dual ligands for the D 2 and 5-HT 1A receptors from the group of 1,8-naphthyl derivatives of LCAP. Article Snippet: Accepted Manuscript New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP Przemysław Zaręba, Jolanta Jaśkowska, Paweł Śliwa, Grzegorz Satała PII: S0960-894X(19)30409-3 DOI: https://doi.org/10.1016/j.bmcl.2019.06.029 Reference: BMCL 26507 To appear in: Bioorganic & Medicinal Chemistry Letters Received Date: 7 May 2019 Revised Date: 17 June 2019 Accepted Date: 19 June 2019 Please cite this article as: Zaręba, P., Jaśkowska, J., Śliwa, P., Satała, G., New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP, Bioorganic & Medicinal Chemistry Letters (2019), doi: https://doi.org/10.1016/j.bmcl.2019.06.029 This is a PDF file of an unedited manuscript that has been accepted for publication.. As a service to our customers we are providing this early version of the manuscript.. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Article Title: A dual-acting 5-HT6 receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties Article Snippet: .. HEK293 cells stably expressing human 5-HT1A, 5-HT6, 5-HT7b and D2L receptors (prepared with the use of Lipofectamine 2000) or CHOeK1 cells with plasmid containing the sequence coding for the Article Title: Dual 5-HT 6 and D 3 Receptor Antagonists in a Group of 1 H -Pyrrolo[3,2- c ]quinolines with Neuroprotective and Procognitive Activity. Article Snippet: .. Cell culture and preparation of cell membranes for radioligand binding assays All the experiments were carried our according to the previously published procedures.32,51,52 HEK293 cells with stable expression of human 5-HT1A, 5-HT2A, 5-HT6, 5- HT7b and D2L receptors (prepared with the use of Lipofectamine 2000) or CHO-K1 cells with plasmid containing the sequence coding for the Plasmid Preparation:Article Title: Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants Article Snippet: Accepted Manuscript Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants Przemysław Zaręba, Jolanta Jaśkowska, Izabela Czekaj, Grzegorz Satała PII: S0968-0896(19)30783-7 DOI: https://doi.org/10.1016/j.bmc.2019.06.028 Reference: BMC 14965 To appear in: Bioorganic & Medicinal Chemistry Received Date: 9 May 2019 Revised Date: 17 June 2019 Accepted Date: 18 June 2019 Please cite this article as: Zaręba, P., Jaśkowska, J., Czekaj, I., Satała, G., Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants, Bioorganic & Medicinal Chemistry (2019), doi: https://doi.org/10.1016/j.bmc.2019.06.028 This is a PDF file of an unedited manuscript that has been accepted for publication.. As a service to our customers we are providing this early version of the manuscript.. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Article Title: N-Skatyltryptamines—Dual 5-HT6R/D2R Ligands with Antipsychotic and Procognitive Potential Article Snippet: .. HEK293 cells (ATCC) with the stable expression of human serotonin 5-HT1AR, 5-HT6, and 5-HT7bR or dopamine D2LR (obtained using of Lipofectamine 2000, Invitrogen) or CHO-K1 cells with plasmid containing the sequence coding for the Article Title: Chlorine substituents and linker topology as factors of 5-HT6R activity for novel highly active 1,3,5-triazine derivatives with procognitive properties in vivo Article Snippet: .. HEK293 cells with stable expression of human 5-HT6, 5-HT7b and D2L receptors (prepared with the use of Lipofectamine 2000) or CHO-K1 cells with plasmid containing the sequence coding for the Article Title: Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs Article Snippet: .. CHO-K1 cells, with plasmid containing the sequence coding for the Article Title: New dual ligands for the D 2 and 5-HT 1A receptors from the group of 1,8-naphthyl derivatives of LCAP. Article Snippet: Accepted Manuscript New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP Przemysław Zaręba, Jolanta Jaśkowska, Paweł Śliwa, Grzegorz Satała PII: S0960-894X(19)30409-3 DOI: https://doi.org/10.1016/j.bmcl.2019.06.029 Reference: BMCL 26507 To appear in: Bioorganic & Medicinal Chemistry Letters Received Date: 7 May 2019 Revised Date: 17 June 2019 Accepted Date: 19 June 2019 Please cite this article as: Zaręba, P., Jaśkowska, J., Śliwa, P., Satała, G., New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP, Bioorganic & Medicinal Chemistry Letters (2019), doi: https://doi.org/10.1016/j.bmcl.2019.06.029 This is a PDF file of an unedited manuscript that has been accepted for publication.. As a service to our customers we are providing this early version of the manuscript.. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Article Title: A dual-acting 5-HT6 receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties Article Snippet: .. HEK293 cells stably expressing human 5-HT1A, 5-HT6, 5-HT7b and D2L receptors (prepared with the use of Lipofectamine 2000) or CHOeK1 cells with plasmid containing the sequence coding for the Article Title: 2-Aminoimidazole-based antagonists of the 5-HT6 receptor – A new concept in aminergic GPCR ligand design Article Snippet: A new strategy in the design of aminergic GPCR ligands is proposed – the use of heterocyclic basic moieties in place of the evergreen piperazine or alicyclic and aliphatic amines.. This hypothesis has been tested using a benchmark series of 5-HT6R antagonists obtained by coupling variously substituted 2-aminoimidazole moieties to the well established 1-benzenesulfonyl-1H-indoles, which served as the ligands cores.. The crystallographic studies revealed that upon protonation, the 2-aminoimidazole fragment triggers a resonance driven conformational change leading to a form of higher affinity. Article Title: Dual 5-HT 6 and D 3 Receptor Antagonists in a Group of 1 H -Pyrrolo[3,2- c ]quinolines with Neuroprotective and Procognitive Activity. Article Snippet: .. Cell culture and preparation of cell membranes for radioligand binding assays All the experiments were carried our according to the previously published procedures.32,51,52 HEK293 cells with stable expression of human 5-HT1A, 5-HT2A, 5-HT6, 5- HT7b and D2L receptors (prepared with the use of Lipofectamine 2000) or CHO-K1 cells with plasmid containing the sequence coding for the Sequencing:Article Title: Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants Article Snippet: Accepted Manuscript Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants Przemysław Zaręba, Jolanta Jaśkowska, Izabela Czekaj, Grzegorz Satała PII: S0968-0896(19)30783-7 DOI: https://doi.org/10.1016/j.bmc.2019.06.028 Reference: BMC 14965 To appear in: Bioorganic & Medicinal Chemistry Received Date: 9 May 2019 Revised Date: 17 June 2019 Accepted Date: 18 June 2019 Please cite this article as: Zaręba, P., Jaśkowska, J., Czekaj, I., Satała, G., Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants, Bioorganic & Medicinal Chemistry (2019), doi: https://doi.org/10.1016/j.bmc.2019.06.028 This is a PDF file of an unedited manuscript that has been accepted for publication.. As a service to our customers we are providing this early version of the manuscript.. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Article Title: N-Skatyltryptamines—Dual 5-HT6R/D2R Ligands with Antipsychotic and Procognitive Potential Article Snippet: .. HEK293 cells (ATCC) with the stable expression of human serotonin 5-HT1AR, 5-HT6, and 5-HT7bR or dopamine D2LR (obtained using of Lipofectamine 2000, Invitrogen) or CHO-K1 cells with plasmid containing the sequence coding for the Article Title: Chlorine substituents and linker topology as factors of 5-HT6R activity for novel highly active 1,3,5-triazine derivatives with procognitive properties in vivo Article Snippet: .. HEK293 cells with stable expression of human 5-HT6, 5-HT7b and D2L receptors (prepared with the use of Lipofectamine 2000) or CHO-K1 cells with plasmid containing the sequence coding for the Article Title: Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs Article Snippet: .. CHO-K1 cells, with plasmid containing the sequence coding for the Article Title: New dual ligands for the D 2 and 5-HT 1A receptors from the group of 1,8-naphthyl derivatives of LCAP. Article Snippet: Accepted Manuscript New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP Przemysław Zaręba, Jolanta Jaśkowska, Paweł Śliwa, Grzegorz Satała PII: S0960-894X(19)30409-3 DOI: https://doi.org/10.1016/j.bmcl.2019.06.029 Reference: BMCL 26507 To appear in: Bioorganic & Medicinal Chemistry Letters Received Date: 7 May 2019 Revised Date: 17 June 2019 Accepted Date: 19 June 2019 Please cite this article as: Zaręba, P., Jaśkowska, J., Śliwa, P., Satała, G., New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP, Bioorganic & Medicinal Chemistry Letters (2019), doi: https://doi.org/10.1016/j.bmcl.2019.06.029 This is a PDF file of an unedited manuscript that has been accepted for publication.. As a service to our customers we are providing this early version of the manuscript.. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Article Title: A dual-acting 5-HT6 receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties Article Snippet: .. HEK293 cells stably expressing human 5-HT1A, 5-HT6, 5-HT7b and D2L receptors (prepared with the use of Lipofectamine 2000) or CHOeK1 cells with plasmid containing the sequence coding for the Article Title: 2-Aminoimidazole-based antagonists of the 5-HT6 receptor – A new concept in aminergic GPCR ligand design Article Snippet: A new strategy in the design of aminergic GPCR ligands is proposed – the use of heterocyclic basic moieties in place of the evergreen piperazine or alicyclic and aliphatic amines.. This hypothesis has been tested using a benchmark series of 5-HT6R antagonists obtained by coupling variously substituted 2-aminoimidazole moieties to the well established 1-benzenesulfonyl-1H-indoles, which served as the ligands cores.. The crystallographic studies revealed that upon protonation, the 2-aminoimidazole fragment triggers a resonance driven conformational change leading to a form of higher affinity. Article Title: Dual 5-HT 6 and D 3 Receptor Antagonists in a Group of 1 H -Pyrrolo[3,2- c ]quinolines with Neuroprotective and Procognitive Activity. Article Snippet: .. Cell culture and preparation of cell membranes for radioligand binding assays All the experiments were carried our according to the previously published procedures.32,51,52 HEK293 cells with stable expression of human 5-HT1A, 5-HT2A, 5-HT6, 5- HT7b and D2L receptors (prepared with the use of Lipofectamine 2000) or CHO-K1 cells with plasmid containing the sequence coding for the Modification:Article Title: N-Skatyltryptamines—Dual 5-HT6R/D2R Ligands with Antipsychotic and Procognitive Potential Article Snippet: .. HEK293 cells (ATCC) with the stable expression of human serotonin 5-HT1AR, 5-HT6, and 5-HT7bR or dopamine D2LR (obtained using of Lipofectamine 2000, Invitrogen) or CHO-K1 cells with plasmid containing the sequence coding for the Article Title: A dual-acting 5-HT6 receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties Article Snippet: .. HEK293 cells stably expressing human 5-HT1A, 5-HT6, 5-HT7b and D2L receptors (prepared with the use of Lipofectamine 2000) or CHOeK1 cells with plasmid containing the sequence coding for the Article Title: 2-Aminoimidazole-based antagonists of the 5-HT6 receptor – A new concept in aminergic GPCR ligand design Article Snippet: A new strategy in the design of aminergic GPCR ligands is proposed – the use of heterocyclic basic moieties in place of the evergreen piperazine or alicyclic and aliphatic amines.. This hypothesis has been tested using a benchmark series of 5-HT6R antagonists obtained by coupling variously substituted 2-aminoimidazole moieties to the well established 1-benzenesulfonyl-1H-indoles, which served as the ligands cores.. The crystallographic studies revealed that upon protonation, the 2-aminoimidazole fragment triggers a resonance driven conformational change leading to a form of higher affinity. Stable Transfection:Article Title: A dual-acting 5-HT6 receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties Article Snippet: .. HEK293 cells stably expressing human 5-HT1A, 5-HT6, 5-HT7b and D2L receptors (prepared with the use of Lipofectamine 2000) or CHOeK1 cells with plasmid containing the sequence coding for the Article Title: 2-Aminoimidazole-based antagonists of the 5-HT6 receptor – A new concept in aminergic GPCR ligand design Article Snippet: A new strategy in the design of aminergic GPCR ligands is proposed – the use of heterocyclic basic moieties in place of the evergreen piperazine or alicyclic and aliphatic amines.. This hypothesis has been tested using a benchmark series of 5-HT6R antagonists obtained by coupling variously substituted 2-aminoimidazole moieties to the well established 1-benzenesulfonyl-1H-indoles, which served as the ligands cores.. The crystallographic studies revealed that upon protonation, the 2-aminoimidazole fragment triggers a resonance driven conformational change leading to a form of higher affinity. |