Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Mutational analysis and molecular modelling of the antagonist SR 144528 binding site on the human cannabinoid CB(2) receptor.

European journal of pharmacology - 28 Jul 2000

Gouldson P, Calandra B, Legoux P, Kernéis A, Rinaldi-Carmona M, Barth F, Le Fur G, Ferrara P, Shire D

Abstract excerpt

We have investigated the binding site of the subtype specific antagonist SR 144528, (N-[(1S)-endo-1,3,3-trimethyl bicyclo [2.2. 1]heptan-2-yl]-5-(4-chloro-3-methylphenyl)-1-(4-methoxybenzyl)- pyrazo le-3-carboxamide) on the human cannabinoid CB(2) receptor based on functional studies with mutated receptors. Two serine residues in the fourth transmembrane region, Ser(161) and Ser(165), were singly mutated to the...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Benzoxazines
Share to Binding, Competitive

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Cyclohexanols

Share to Luciferases

Share to Morpholines

Share to Naphthalenes

Share to Pyrazoles

Share to Receptors, Drug

Source

Identifiers

PMID: 10915832
DOI: 10.1016/s0014-2999(00)00439-8

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Mutational analysis and molecular modelling of the antagonist SR 144528 binding site on the human cannabinoid CB(2) receptor.PMID 10915832Read ↗

Role of a conserved lysine residue in the peripheral cannabinoid receptor (CB2): evidence for subtype specificity.Semantic proximity Read ↗

Mutation studies of Ser7.39 and Ser2.60 in the human CB1 cannabinoid receptor: evidence for a serine-induced bend in CB1 transmembrane helix 7.Semantic proximity Read ↗

Targeting the cannabinoid CB2 receptor: mutations, modeling and development of CB2 selective ligands.Semantic proximity Read ↗

Site-directed mutagenesis of the putative human muscarinic M2 receptor binding site.Semantic proximity Read ↗

Ligand binding and modulation of cyclic AMP levels depend on the chemical nature of residue 192 of the human cannabinoid receptor 1.Semantic proximity Read ↗

Determination of the Negative Allosteric Binding Site of Cannabidiol at the CB1 Receptor: A Combined Computational and Site-Directed Mutagenesis StudySemantic proximity Read ↗

Functional characterization of putative cholesterol binding sequence (CRAC) in human type-1 cannabinoid receptor.Semantic proximity Read ↗

Identification of an amino acid residue important for binding of methiothepin and sumatriptan to the human 5-HT(1B) receptor.Semantic proximity Read ↗

Mutation of a conserved serine in TM4 of opioid receptors confers full agonistic properties to classical antagonists.Semantic proximity Read ↗

Evidence that interspecies polymorphism in the human and rat cholecystokinin receptor-2 affects structure of the binding site for the endogenous agonist cholecystokinin.Semantic proximity Read ↗

Structural mimicry in class A G protein-coupled receptor rotamer toggle switches: the importance of the F3.36(201)/W6.48(357) interaction in cannabinoid CB1 receptor activation.Semantic proximity Read ↗

Ligand-binding architecture of human CB2 cannabinoid receptor: evidence for receptor subtype-specific binding motif and modeling GPCR activation.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.