(-)-7'-Isothiocyanato-11-hydroxy-1',1'-dimethylheptylhexahydrocannabinol (AM841), a high-affinity electrophilic ligand, interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor.
about
Minireview: From the bench, toward the clinic: therapeutic opportunities for cannabinoid receptor modulationEndogenous lipid activated G protein-coupled receptors: emerging structural features from crystallography and molecular dynamics simulationsStructural biology of human cannabinoid receptor-2 helix 6 in membrane-mimetic environmentsUnderstanding functional residues of the cannabinoid CB1.Design and synthesis of novel prostaglandin E2 ethanolamide and glycerol ester probes for the putative prostamide receptor(s)Biochemical and mass spectrometric characterization of human N-acylethanolamine-hydrolyzing acid amidase inhibitionTerpenes and lipids of the endocannabinoid and transient-receptor-potential-channel biosignaling systemsLigand-binding architecture of human CB2 cannabinoid receptor: evidence for receptor subtype-specific binding motif and modeling GPCR activation.Mass spectrometry-based proteomics of human cannabinoid receptor 2: covalent cysteine 6.47(257)-ligand interaction affording megagonist receptor activation.Mapping Cannabinoid 1 Receptor Allosteric Site(s): Critical Molecular Determinant and Signaling Profile of GAT100, a Novel, Potent, and Irreversibly Binding Probe.The expression level of CB1 and CB2 receptors determines their efficacy at inducing apoptosis in astrocytomas.Minireview: recent developments in the physiology and pathology of the lysophosphatidylinositol-sensitive receptor GPR55.High-resolution crystal structure of the human CB1 cannabinoid receptor.hCB2 ligand-interaction landscape: cysteine residues critical to biarylpyrazole antagonist binding motif and receptor modulation.2012 Division of medicinal chemistry award address. Trekking the cannabinoid road: a personal perspectiveA lipid pathway for ligand binding is necessary for a cannabinoid G protein-coupled receptorEndocannabinoid binding to the cannabinoid receptors: what is known and what remains unknown.Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).Crystal Structure of the Human Cannabinoid Receptor CB1.The role of Cysteine 6.47 in class A GPCRs(4-(Bis(4-fluorophenyl)methyl)piperazin-1-yl)(cyclohexyl)methanone hydrochloride (LDK1229): a new cannabinoid CB1 receptor inverse agonist from the class of benzhydryl piperazine analogs.Endocannabinoid tone versus constitutive activity of cannabinoid receptors.Cannabinoids alleviate experimentally induced intestinal inflammation by acting at central and peripheral receptors.Identification of essential cannabinoid-binding domains: structural insights into early dynamic events in receptor activationAM841, a covalent cannabinoid ligand, powerfully slows gastrointestinal motility in normal and stressed mice in a peripherally restricted manner.3'-functionalized adamantyl cannabinoid receptor probes.Molecular-interaction and signaling profiles of AM3677, a novel covalent agonist selective for the cannabinoid 1 receptor.Computational Prediction and Biochemical Analyses of New Inverse Agonists for the CB1 ReceptorLong lasting MDM2/Translocator protein modulator: a new strategy for irreversible apoptosis of human glioblastoma cells.Development of novel tail-modified anandamide analogs.Mass spectrometry-based GPCR proteomics: comprehensive characterization of the human cannabinoid 1 receptor.Solid-state NMR and molecular dynamics characterization of cannabinoid receptor-1 (CB1) helix 7 conformational plasticity in model membranesIn vitro and non-invasive in vivo effects of the cannabinoid-1 receptor agonist AM841 on gastrointestinal motor function in the rat.Discriminative stimulus functions in rats of AM1346, a high-affinity CB1R selective anandamide analog.Transmembrane helical domain of the cannabinoid CB1 receptor.The membrane proximal region of the cannabinoid receptor CB1 N-terminus can allosterically modulate ligand affinity.Chromenopyrazole, a Versatile Cannabinoid Scaffold with in Vivo Activity in a Model of Multiple Sclerosis.Molecular Targets of the Phytocannabinoids: A Complex Picture.Distinct second extracellular loop structures of the brain cannabinoid CB(1) receptor: implication in ligand binding and receptor functionLipid bilayer molecular dynamics study of lipid-derived agonists of the putative cannabinoid receptor, GPR55
P2860
Q26829111-EBD9DC12-CB2B-48C9-99E9-F5F81664F92FQ27009220-EAA8446B-4341-4B50-A1A9-911314D44991Q27655311-41CEAE21-E341-43D7-B98A-D80A945C63FBQ27687653-D0C73B6A-3824-4E10-9A51-94960F864FF1Q28261821-E5CBA09D-5AF5-4678-82C8-889E9044DA84Q28483214-97A26E14-0C17-4A88-AE44-E73545A19F74Q28829964-2882F91C-C8F1-4FB7-A8E5-AB05BF05397DQ30373403-6D83B82D-8074-4306-9979-287A9D750213Q30406301-957FDE93-873B-4AB1-A914-C645402E6315Q30842363-96E2B3A2-81D8-4FD9-8021-76A32B9F37D8Q33525520-6F3498B3-AACA-416F-8F89-D2CD21C68FFEQ33636763-7377E540-D23F-4F2F-80EC-758BB17CC81BQ33694212-F33E1357-71A7-46A7-AEB0-C2A03445F697Q33733994-9244DC21-9773-453C-B8F6-BA47AE6B2CA2Q33781776-D11325BD-4767-4069-9B14-109BA9DC8551Q33885350-80EB36DC-E798-45CF-82F5-7EF6342C7371Q33997873-9B782E98-B02A-4E42-ABA5-EE2F501A3824Q34500324-D6B65CDE-9133-47DC-8DA2-0EB5EE8CCFA4Q34543208-8C126613-6BE0-4FFF-9E29-EF43D636594EQ34623053-E5C5BD01-A716-4CA4-B2BB-12C3B4D97AE0Q34946743-0309ED0D-C267-4A3F-94A8-8A7351E3B303Q35193265-9047725D-EDA0-4F40-B676-0BFD0FD94CD4Q35294138-10258BB5-88BE-4288-84FE-3C5FC2C7EBDAQ35312313-B814CC46-E1A2-4189-B71E-5F660E7BD972Q35484505-20C55A40-57C0-4B53-BC39-53C251E36D88Q35586643-D26FB88D-0E96-40F5-9F9B-4FAAADE8D37DQ36720905-7089CBC8-B80D-4F0E-AF63-592C7CF72D9CQ36890833-103C4EAA-52DE-4D2F-ABEA-20DF37486C35Q36946655-8925D42A-830E-4B8C-8A3E-11D4FC706214Q36956799-E0B992D9-F42C-41D2-B0FC-705B0D7C1F21Q36971376-51EA1C87-6798-4217-845E-D6D90D709C2DQ37016808-96BEF828-3309-44D1-BC47-C683174566D6Q37032490-A6E0AA84-53CB-4F63-9A79-87C0D599DF8FQ37055254-195FD94F-AB57-4E09-9B41-5135CACA36E7Q37282203-794B0BAE-4539-4065-999A-4B1787482BE0Q37609921-866D34F9-CC2A-4F4E-8615-7D4E75C341CEQ37659341-1997D20A-69BE-4BAB-9FB7-09214FD36F71Q37692746-0992616D-1C98-475B-8F1D-0EBBA3841105Q42694873-C19F4A0D-00F0-4182-8A30-46EF8FFEB315Q42725727-95204E56-3EF9-463E-A14F-DEE8A533AAF4
P2860
(-)-7'-Isothiocyanato-11-hydroxy-1',1'-dimethylheptylhexahydrocannabinol (AM841), a high-affinity electrophilic ligand, interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor.
description
2005 nî lūn-bûn
@nan
2005年の論文
@ja
2005年学术文章
@wuu
2005年学术文章
@zh-cn
2005年学术文章
@zh-hans
2005年学术文章
@zh-my
2005年学术文章
@zh-sg
2005年學術文章
@yue
2005年學術文章
@zh
2005年學術文章
@zh-hant
name
(-)-7'-Isothiocyanato-11-hydro ...... the CB1 cannabinoid receptor.
@en
(-)-7'-Isothiocyanato-11-hydro ...... the CB1 cannabinoid receptor.
@nl
type
label
(-)-7'-Isothiocyanato-11-hydro ...... the CB1 cannabinoid receptor.
@en
(-)-7'-Isothiocyanato-11-hydro ...... the CB1 cannabinoid receptor.
@nl
prefLabel
(-)-7'-Isothiocyanato-11-hydro ...... the CB1 cannabinoid receptor.
@en
(-)-7'-Isothiocyanato-11-hydro ...... the CB1 cannabinoid receptor.
@nl
P2093
P921
P356
P1476
(-)-7'-Isothiocyanato-11-hydro ...... the CB1 cannabinoid receptor.
@en
P2093
Atmaram D Khanolkar
Donna J Fournier
Dow P Hurst
Ganesh A Thakur
Lionel A Ayotte
Patricia H Reggio
Robert P Picone
P304
P356
10.1124/MOL.105.014407
P577
2005-09-12T00:00:00Z