• 2MbisP binds to the receptor despite the absence of the 25-hydroxyl group. (rcsb.org)
  • Evidence suggests that C1q binds a receptor present on phagocytic cells, termed C1qRP. (medscape.com)
  • The C3a receptor binds C3a and C4a. (medscape.com)
  • Also, the homologous histamine receptor (HisR) from Apis mellifera was investigated to understand how histamine binds and relate this binding to potentially mislabelled receptors in mammals. (dundee.ac.uk)
  • When a ligand binds to the Notch2 receptor, it triggers signals that are important for the normal development and function of many different types of cells. (medlineplus.gov)
  • 7 The differential reductions in the potencies of SLIGRL-NH2, compared with trypsin in the PAR2PRR and PAR2NET cell lines point to differences between the interactions of the trypsin-revealed tethered ligand and the free receptor-activating peptide with PAR2. (nih.gov)
  • A comparison of these structures with existing ER structures suggests that the ERbeta selectivity of OBCP ligands can be attributed to a combination of their interactions with Met-336 in ERbeta and Met-421 in ERalpha. (rcsb.org)
  • Binding of the 2-carbon-modified analogues does not change the positions of the amino acids in the ligand binding site and has no effect on the interactions in the coactivator binding pocket. (rcsb.org)
  • Electrostatic and hydrophobic interactions between the peptide and the LBD stabilize the active receptor conformation. (rcsb.org)
  • The present study used in vitro expression systems to investigate interactions of members of the KDN series with δ-κ heterodimers through competition binding using selective ligands and the mitogen-activated protein kinase (MAPK) assay. (aspetjournals.org)
  • Although the mechanism of action of ibogaine, a hallucinogen that may be useful in the treatment of addiction, remains unknown, receptor binding studies suggest that ibogaine produces its effects via interactions with multiple receptor types. (erowid.org)
  • In an attempt to determine which of these receptor interactions are involved in the in vivo effects of ibogaine, ligands for sigma, PCP, and opiate receptors were assessed for their ability to substitute for or to antagonize the ibogaine-induced discriminative stimulus (10 mg/kg I.P., 60 min presession) in Fischer-344 rats. (erowid.org)
  • In contrast to sigma2 and opiate receptors, ibogaine's reported interactions with NMDA receptors do not appear to be involved in its discriminative stimulus, as neither PCP nor MK-801 produced a significant level of ibogaine-appropriate responding. (erowid.org)
  • scDiffCom is an R package, relying on approximately 5,000 curated ligand-receptor interactions, that performs differential intercellular communication analysis between two conditions from single-cell transcriptomics data. (nature.com)
  • Data from the study of N-methylbicuculline suggest that it is promiscuous due to the flexibility of the orthosteric binding site of pLGIC members as well as the number of interactions the ligand can form, therefore a favourable orientation can always be adopted. (dundee.ac.uk)
  • Investigation of these ligands could further understanding of protein-ligand interactions with GBP and AcAChBP, as well as the physiological receptors GlyR and nAChR. (dundee.ac.uk)
  • In this study, we have characterized a novel approach for identification and selection of protein-protein interactions, denoted SPIRE (selection of protein interactions by receptor engagement), which is based on a mammalian expression system. (lu.se)
  • Toll-like receptors (TLRs) are transmembrane proteins involved in innate immune response. (irb.hr)
  • Comparative functional multiomics showed that blood proteins induce distinct receptor-mediated transcriptional programs in microglia and macrophages, such as redox, type I interferon and lymphocyte recruitment. (nature.com)
  • We report a blood-induced microglia gene network and show that blood proteins elicit distinct receptor-mediated transcriptional changes and signaling programs in innate immune cells. (nature.com)
  • This study assessed 80 cardiovascular and inflammatory proteins for biomarker discovery and prediction of MACE in type 2 diabetes. (springer.com)
  • We combined data from six prospective epidemiological studies of 30-77-year-old individuals with type 2 diabetes in whom 80 circulating proteins were measured by proximity extension assay. (springer.com)
  • 5% false discovery rate) between risk of MACE and eight proteins: matrix metalloproteinase (MMP)-12, IL-27 subunit α (IL-27a), kidney injury molecule (KIM)-1, fibroblast growth factor (FGF)-23, protein S100-A12, TNF receptor (TNFR)-1, TNFR-2 and TNF-related apoptosis-inducing ligand receptor (TRAIL-R)2. (springer.com)
  • The screens were conducted to discover new ligands of the proteins. (dundee.ac.uk)
  • Receptor proteins have specific sites into which certain other proteins, called ligands, fit like keys into locks. (medlineplus.gov)
  • citation needed] Diihydrochloride salts of DREADDs ligands that are water-soluble (but with differing stabilities in solution) have also been commercially developed (see for aqueous stability). (wikipedia.org)
  • The aim of this study is to investigate the insulin-like growth factor type 2 (IGF2R) gene and circulating soluble IGF2R in relation to type 2 diabetes (T2DM). (hindawi.com)
  • RÉSUMÉ L'objectif de l'étude était d'évaler l'importance clinique du ligand de CD40 soluble (sCD40L) chez des patients atteints d'un carcinome hépatocellulaire (CHC) associé au virus de l'hépatite C (VHC). (who.int)
  • From the screen, we identified a family of ERbeta-selective agonists whose members contain bulky oxabicyclic scaffolds in place of the planar scaffolds common to most ER ligands. (rcsb.org)
  • Regarding the selectivity of KDN21 for phenotypic δ and κ opioid receptors, we investigated the effect of KDN21 on the activation of MAPKs [extracellular signal-regulated kinases 1 and 2 (ERK1/2)] by δ- or κ-selective agonists. (aspetjournals.org)
  • The results of studies with selective agonists and antagonists in vivo are consistent with cooperativity between δ and κ receptors, and it has been proposed that the putative δ 1 and κ 2 opioid receptor subtypes are actually phenotypes ( Portoghese and Lunzer, 2003 ). (aspetjournals.org)
  • With regard to opiate receptors, neither morphine, the prototypic mu agonist, nor kappa selective agonists (bremazocine,and U-50488) substituted for ibogaine. (erowid.org)
  • These receptors are also known as GsD and are chimeric receptors containing intracellular regions of the turkey erythrocyte β-adrenergic receptor substituted into the rat M3 DREADD. (wikipedia.org)
  • It is of note that rather than mediating intracellular signaling transduction elicited by IGF2, the IGF type 2 receptor (IGF2R) acts as a IGF2 scavenger. (hindawi.com)
  • intracellular receptors. (muni.cz)
  • Our results indicate that context-dependent recruitment of alternative intracellular signaling pathways within a single sensory neuron type conveys opposite hedonic valences, thereby providing a robust mechanism for odorant encoding and discrimination at the periphery. (plos.org)
  • To provide insight into the molecular mechanisms of their activity and selectivity, we determined the crystal structures of the ERalpha ligand-binding domain (LBD) and a peptide from the glucocorticoid receptor-interacting protein 1 (GRIP1) coactivator complexed with the ligands OBCP-3M, OBCP-2M, and OBCP-1M. (rcsb.org)
  • Divergent Ah receptor ligand selectivity during hominin evolution. (oregonstate.edu)
  • This property allows SARMs the advantage of androgen-receptor specificity, tissue selectivity, and the lack of steroid-related side effects. (medium.com)
  • Homeostatic osteoclastogenesis is effectively induced by RANKL (Receptor activator of nuclear factor kappa-B ligand). (frontiersin.org)
  • Moreover, ISE up-regulated the osteoprotegerin/receptor activator of nuclear factor κB ligand ratio. (degruyter.com)
  • Prolia works by blocking a protein called RANK (receptor activator of nuclear factor kappa beta) and helps prevent bone cells called osteoclasts from breaking down bone in the body. (medlineplus.gov)
  • Ligand binding induces conformational changes that allow ions to flow through a pore generated by the TMD. (dundee.ac.uk)
  • Neonatal exposure to a Type-I pyrethroid (bioallethrin) induces dose-response changes in brain muscarinic receptors and behaviour in neonatal and adult mice. (cdc.gov)
  • This chemogenetic technique can be used for remote manipulation of cells, in particular excitable cells like neurons, both in vitro and in vivo with the administration of specific ligands. (wikipedia.org)
  • Our analysis emphasizes the relevance of the specific ligands, receptors and cell types regulating these processes. (nature.com)
  • Specific receptors on cell membranes that react with PLATELET-DERIVED GROWTH FACTOR, its analogs, or antagonists. (bvsalud.org)
  • Click on one of the subfamilies of IgSF or TNFRSF co-signaling receptors shown in the Explore Pathways box below to see how the different members of each family affect T cell activation. (rndsystems.com)
  • We provide a transcriptomic and phosphoproteomic atlas of fibrin-, iC3b- and lipopolysaccharide (LPS)-selective activation of innate immunity and reveal ligand-selective pathways with differential functions in MS and AD mice. (nature.com)
  • ancestral variant) in the ligand-binding domain of the aryl hydrocarbon receptor (AHR) gene. (oregonstate.edu)
  • Benzimidazoisoquinolines: a new class of rapidly metabolized aryl hydrocarbon receptor (AhR) ligands that induce AhR-dependent Tregs and prevent murine graft-versus-host disease. (oregonstate.edu)
  • The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor that plays multiple roles in regulation of immune and inflammatory responses. (oregonstate.edu)
  • Activation of the protein-tyrosine kinase activity of the receptors occurs by ligand-induced dimerization or heterodimerization of PDGF receptor types. (bvsalud.org)
  • We assessed the efficacy and potency of structurally distinct KOR small molecule and peptide ligands. (ku.edu)
  • These receptors, a subset of the Class A/1 (Rhodopsin-like) family, all bind peptide ligands which include the chemokines, opioids and somatostatins. (reactome.org)
  • These systems typically utilize G protein-coupled receptors (GPCR) engineered to respond exclusively to synthetic ligands, like clozapine N-oxide (CNO), and not to endogenous ligands. (wikipedia.org)
  • These engineered GPCRs are unresponsive to endogenous ligands but can be activated by nanomolar concentrations of pharmacologically inert, drug-like small molecules. (wikipedia.org)
  • In this project we will explore the role of TLR3 activation in cancer development by focusing on the role of its endogenous ligands. (irb.hr)
  • We will study this on several models: a) TLR3 reporter cell line HEK-Blue to validate the in vivo and in vitro existence of TLR3 endogenous ligands derived from necrotic cells and tissue, b) head and neck cancer cell lines stably transfected with shRNA for TLR3 and c) cancer tissue specimens isolated from head and neck cancer patients. (irb.hr)
  • Second approach will include studying the role of TLR3 and its endogenous ligands in cancer stem cells (CSC) development and self-renewal. (irb.hr)
  • Our approach will include combining proton or gamma-ray irradiation with the treatment with poly (I:C) and pharmacological inhibitors of endogenous ligands. (irb.hr)
  • Here, we report that the recently sequenced genome from the red flour beetle Tribolium castaneum contains a gene coding for an oxytocin/vasopressin-like peptide, identical to the locust peptide, which we named inotocin (for insect oxytocin/vasopressin-like peptide) and a gene coding for an inotocin G protein-coupled receptor (GPCR). (lu.se)
  • This GPCR is strongly activated by low concentrations of inotocin (EC 50 , 5 × 10 -9 M), demonstrating that it is the inotocin receptor. (lu.se)
  • RASSLs and DREADDs are families of designer G-protein-coupled receptors (GPCRs) built specifically to allow for precise spatiotemporal control of GPCR signaling in vivo. (wikipedia.org)
  • The multi-functional class A macrophage scavenger receptor (SRA)/CD204 has emerged as an important class of pattern recognition receptors with broad ligand binding ability. (cdc.gov)
  • The weak uterotrophic activity of these ligands in immature rats and their ability to stimulate expression of an ERbeta regulated gene in human U2OS osteosarcoma cells provides more physiological evidence of their ERbeta-selective nature. (rcsb.org)
  • Immunization studies in female rats demonstrated that Fusion-FD12 immune sera , but not purified IgG , neutralized vaccine -type parasites more efficiently compared to apoAMA1, despite lower overall anti-AMA1 titers. (bvsalud.org)
  • M1 and M5 muscarinic receptors have been mutated to create DREADDs hM1Dq and hM5Dq respectively. (wikipedia.org)
  • Determining the function of CMV-encoded chemokine receptors in the context of viral pathogenesis and acceleration of vascular disease. (ohsu.edu)
  • Activation of PERK affects innate immunity by suppression of type 1 interferon (IFN) signaling. (nih.gov)
  • ligand binding potency and activation of several groups of major semi-volatile organic compounds (SVOCs) that are ubiquitously detected in indoor environments, including flame retardants such as polybrominated diphenyl ethers (PBDEs) and Firemaster 550 (FM550), and other SVOCs such as phthalates, organotins, halogenated phenols and bisphenols. (duke.edu)
  • Binding of these ligands to RAGE does not accelerate clearance or degradation but rather begins a sustained period of cellular activation mediated by receptor-dependent signaling. (jci.org)
  • These differences have stimulated the search for subtype-selective ligands. (rcsb.org)
  • In this regard, the use of the selective radioligands [ 3 H]naltrindole and [ 3 H]norbinaltorphimine (nor-BNI) in competition binding studies revealed that KDN21 has much higher affinity than other KDN members for CDK and bound to CDK more selectively relative to mixed δ and κ opioid receptors or singly expressed δ and κ opioid receptors. (aspetjournals.org)
  • Intermediate levels of generalization were observed with the subtype nonselective sigma ligands 3-(3-hydroxyphenyl)-N-(1-propyl)-piperidine [(+)-3-PPP] (69.0%) and 1,3-di(2-tolyl)guanidine (DTG) (73.5%) but not with the sigma1-selective agents (+)-N-allylnormetazocine [(+)-SKF 10,047] and (+)-pentazocine. (erowid.org)
  • The aim of the present study was to test and compare effects of often used selective Sig1R ligands in models of experimentally induced seizures. (rsu.lv)
  • MK-677, also known as Ibutamoren, is often lumped together with Selective Androgen Receptor Modulators ( SARMs ). (medium.com)
  • MK-677, or Ibutamoren, is a potent, long-acting, orally active, selective, and non-peptide agonist of the ghrelin receptor and a growth hormone secretagogue, mimicking the growth hormone (GH)-stimulating action of the endogenous hormone ghrelin . (medium.com)
  • Selective Androgen Receptor Modulators (SARMs) are a class of therapeutic compounds that have similar properties to anabolic agents, but with reduced androgenic properties . (medium.com)
  • Alternate glucocorticoid receptor ligand binding structures influence outcomes in an in vivo tissue regeneration model. (oregonstate.edu)
  • In vivo assessment of these corticosteroid analogs is essential to understand the difference in molecular signaling of the ligands that share the corticosteroid backbone. (oregonstate.edu)
  • JHU37160 and JHU37152 have been marketed commercially as novel DREADD ligands, active in vivo, with high potency and affinity for hM3Dq and hM4Di DREADDs. (wikipedia.org)
  • Although the in vitro binding data were consistent with the in vivo study, it did not identify the binding characteristics of each of the bridged receptors. (aspetjournals.org)
  • The development of targeted therapies, including prostacyclin analogs, endothelin receptor antagonists, and tyrosine kinase inhibitors, has revolutionized the treatment of PAH. (reportsnreports.com)
  • Newer glucose-lowering drugs such as sodium-glucose co-transporter 2 inhibitors, and cholesterol-modifying agents such as proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors, in addition to standard treatment reduce cardiovascular risk in high-risk individuals [ 8 , 9 ]. (springer.com)
  • Other unusual features of the receptor include its ability to engage classes of molecules, rather than individual ligands, and its enhanced surface expression in environments rich in RAGE ligands. (jci.org)
  • Ligands for CD11a/CD18 are intercellular adhesion molecules (ICAMs), ligands for CD11b/CD18 are complement C3bi and ICAMs, and ligands for CD11c/CD18 are C3bi and ICAMs. (medscape.com)
  • 2. SLIGEL-NH2 exhibited low potency (1 : 200 relative to SLIGRL-NH2) in wild-type PAR2. (nih.gov)
  • 4. In PAR2NET, highly homologous in EL-2 with proteinase-activated receptor-1 (PAR1), the potency of the PAR1-derived peptide, SFLLR-NH2, was reduced by 100 fold compared with wt-PAR2, whereas the potency of the PAR2-derived AP, SLIGRL-NH2 was reduced 10 fold. (nih.gov)
  • These data demonstrate that the FMP assay is a sensitive method for assessing κ-opioid receptor induced hyperpolarization, and represents a useful approach for quantification of potency, efficacy and desensitization of KOR ligands. (ku.edu)
  • Only two point mutations of hM3 were required to achieve a mutant receptor with nanomolar potency for CNO, insensitivity to acetylcholine and low constitutive activity and this DREADD receptor was named hM3Dq. (wikipedia.org)
  • With regard to glucose homeostasis, genetic variants in the IGF2R gene have been shown to be associated with both type 1 [ 5 ] and type 2 diabetes (T2DM) [ 6 ]. (hindawi.com)
  • This gene provides instructions for making a receptor called Notch2. (medlineplus.gov)
  • We performed in silico molecular docking and dynamic studies and demonstrated that type and size of substitution at the C17 position of the cortisol backbone confer a unique stable conformation to GR on ligand binding that is critical for inhibitory activity. (oregonstate.edu)
  • The most commonly used inhibitory DREADD is hM4Di, derived from the M4 muscarinic receptor that couples with the Gi protein. (wikipedia.org)
  • Another inhibitory Gi-DREADD is the kappa-opioid-receptor (KOR) DREADD (KORD) which is selectively activated by salvinorin B (SalB). (wikipedia.org)
  • Cholinergic, adrenergic, and (inhibitory) gabaergic receptors. (muni.cz)
  • We screened a ChemBridge small molecule library and identified 10-chloro-7H-benzimidazo[2,1-a]benzo[de]Iso-quinolin-7-one (10-Cl-BBQ) as a potent AhR ligand that was rapidly metabolized and not cytotoxic to proliferating T cells. (oregonstate.edu)
  • KDN21 is a bivalent ligand that contains δ and κ opioid antagonist pharmacophores linked through a 21-atom spacer. (aspetjournals.org)
  • KDN21 contains δ and κ opioid receptor antagonist pharmacophores that are connected through a 21-atom spacer ( Fig. 1 ). (aspetjournals.org)
  • La activación de la actividad proteín-tirosina cinasa de los receptores tiene lugar por dimerización o heterodimerización de los tipos de receptor de PDGF inducida por ligandos. (bvsalud.org)
  • We explored the utility of the real-time FLIPR Membrane Potential (FMP) assay as a method to assess kappa opioid receptor (KOR)-induced hyperpolarization. (ku.edu)
  • Ligand-specific differences in membrane trafficking of the GLP-1R influence its signalling properties and therapeutic potential in type 2 diabetes. (cam.ac.uk)
  • Of the 8 plasma membrane receptors for complement, only deficiencies of CR3 and CR4 due to CD18 deficiency have been described, known as leukocyte adhesion deficiency (LAD) type 1 . (medscape.com)
  • These membrane receptors convert chemical signals of neurotransmitters into electrical signals of an ion flow, mainly at synapses. (dundee.ac.uk)
  • We have demonstrated proof of concept by creating a general plasma membrane bound decoy receptor, by displaying a protein or a peptide genetically fused to a trunctated version of the CD40 molecule. (lu.se)
  • Pattern recognition scavenger receptor A/CD204 regulates airway inflammatory homeostasis following organic dust extract exposures. (cdc.gov)
  • The 3a protein was found to induce serine phosphorylation within the IFN alpha-receptor subunit 1 (IFNAR1) degradation motif and to increase IFNAR1 ubiquitination. (nih.gov)
  • The ability of certain AhR ligands to induce regulatory T cells (Tregs) has generated interest in developing AhR ligands for therapeutic treatment of immune-mediated diseases. (oregonstate.edu)
  • Our research identified a novel function of GCs as modulators of tissue regeneration and demonstrated that GCs activate the glucocorticoid receptor (GR) to inhibit early stages of tissue regeneration in zebrafish (Danio rerio). (oregonstate.edu)
  • Estrogen receptors alpha (ERalpha) and beta (ERbeta) have distinct functions and differential expression in certain tissues. (rcsb.org)
  • Taken together, these features of RAGE allow the receptor to propagate cellular dysfunction in a number of pathophysiologically relevant situations, most often dictated by the formation and persistence of ligands in the tissues. (jci.org)
  • Overall, the data demonstrate that SRA/CD204 plays an important role in the normative inflammatory lung response to ODE, as evidenced by the enhanced dust-mediated injury viewed in the absence of this receptor. (cdc.gov)
  • whether a distinct receptor for C4a is present is unclear (see Table 1). (medscape.com)
  • The valence of individual chemicals is largely determined by the responding sensory neuron type, such that distinct subsets of chemosensory neurons drive either attraction or avoidance to different chemicals [ 25 , 26 ]. (plos.org)
  • The HIT2 antibody reacts with CD38, an ~45 kDa type II transmembrane glycoprotein expressed by many cell types, especially leukocytes. (stemcell.com)
  • Cell lines were evaluated for their sensitivity (calcium signalling) towards trypsin and the receptor-activating peptides, SLIGRL-NH2, SLIGEL-NH2, trans-cinnamoyl(tc)-LIGRLO-NH2, and SFLLR-NH2. (nih.gov)
  • In contrast, TNF often acts on cell types other than osteoclasts, or synergically with RANKL to indirectly promote osteoclastogenesis and bone resorption. (frontiersin.org)
  • Normal bone remodeling requires a delicate balance between the activities of major bone cell types: bone-resorbing osteoclasts and bone-forming osteoblasts, as well as osteocytes. (frontiersin.org)
  • The ICD is the site of cell- receptor communication. (dundee.ac.uk)
  • Some labile cell types whose numbers are normally or all severe infections that could be targets for pharmaco- controlled through programmed cell death are subject to logic intervention. (cdc.gov)
  • Extensive lymphocyte severe infections is a massive loss of lymphocytes, den- apoptosis has also occurred in humans and animals infect- dritic cells, gastrointestial epithelial cells, and other cell ed with several exotic agents, including Bacillus anthracis , types through apoptosis, or programmed cell death. (cdc.gov)
  • When this decoy receptor is engaged by a ligand to the displayed protein/peptide, the receptor expressing cell is rescued from apoptosis. (lu.se)
  • To design a high-throughput system with a highly parallel capacity, we utilized the B cell line WEHI-231, as carrier of the decoy receptor. (lu.se)
  • One specific peptide-displaying cell could be identified and amplified, based on a specific receptor engagement, in a background of 12 500 wild-type cells after four selections. (lu.se)
  • In Chapter 3, the biophysical techniques surface plasmon resonance (SPR), isothermal titration calorimetry (ITC) and tryptophan fluorescence (WF) were assessed utilising AcAChBP and three of its ligands. (dundee.ac.uk)
  • G-protein-coupled receptors (GPCRs) are typically considered to function as monomers. (aspetjournals.org)
  • Opioid receptors belong to rhodopsin receptor family of GPCRs. (aspetjournals.org)
  • However, the specific ligand of NTHi responsible for this interaction remains unknown. (lu.se)
  • A receptor activated solely by a synthetic ligand (RASSL) or designer receptor exclusively activated by designer drugs (DREADD), is a class of artificially engineered protein receptors used in the field of chemogenetics which are selectively activated by certain ligands. (wikipedia.org)
  • An important step toward this goal would be the development of pharmacological tools that selectively target opioid receptor heterodimers. (aspetjournals.org)
  • SARMs work by selectively binding to androgen receptors in the body. (medium.com)
  • These receptors are present on phagocytic cells, mast cells, and lung epithelial and smooth muscle cells. (medscape.com)
  • The C-Type Lectin receptor (CRL) is known as the major β-glucan receptor expressed in myeloid cells and is responsible for targeting respiratory fungal pathogens. (lu.se)
  • Quantitative RT-PCR (qPCR) showed that in adult Tribolium, the receptor is mainly expressed in the head and much less in the hindgut and Malpighian tubules, suggesting that the inotocin/receptor couple does not play a role in water homeostasis. (lu.se)
  • The glucagon-like peptide-1 receptor (GLP-1R) is an important regulator of blood glucose homeostasis. (cam.ac.uk)
  • CD155, known as poliovirus receptor (PVR) or nectin-like 5, is a 70 kD type I transmembrane glycoprotein. (biolegend.com)
  • CD11c is a 145-150 kD type I transmembrane glycoprotein also known as integrin α x and CR4. (biolegend.com)
  • These ligands originate from necrotic cancer cells and may stimulate cancer progression. (irb.hr)
  • Depending on their chemical structure, they can either block or stimulate these receptors, which can help to promote muscle growth, fat loss, and performance enhancement. (medium.com)
  • We have shown previously that when using [ 3 H]diprenorphine as radioligand, KDN21 displayed greatly enhanced affinity in this series for coexpressed δ and κ opioid receptors (CDK). (aspetjournals.org)
  • These findings, along with observations that ibogaine has appreciable affinity for sigma2 receptors, suggest that these receptors may be involved in the ibogaine discriminative stimulus. (erowid.org)
  • The latter observations taken together with the finding that both nalorphine (>100 microM) and diprenorphine (30 microM) have extremely low affinity for sigma2 receptors, suggest that the ibogaine-appropriate responding produced by these agents is not mediated by sigma2 receptors. (erowid.org)