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BD1031
BD1031 or (R)-2- -(3,4-dichlorophenyl)ethylctahydropyrrolo ,2-ayrazine is a selective sigma receptor agonist, with a reported binding affinity of ''K''i = 1 ± 0.2 nM for the sigma-1 receptor and 80 times selectivity over the sigma-2 receptor. The enantiomer of BD1031 is known as BD1018. Consistent with other reported sigma receptor agonists, BD1031 increases the behavioural toxicity of cocaine in Swiss Webster mice. See also * BD1008 BD1008 or N- -(3,4-dichlorophenyl)ethylN-methyl-1-pyrrolidineethanamine is a selective sigma receptor antagonist, with a reported binding affinity of ''K''i = 2 ± 1 nM for the sigma-1 receptor and 4 times selectivity over the sigma-2 receptor. ... References {{Sigma receptor modulators Sigma agonists ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BD1018
BD1018 or (S)-2- -(3,4-dichlorophenyl)ethylctahydropyrrolo ,2-ayrazine is a selective sigma receptor ligand, with a reported binding affinity of ''K''i = 5 ± 0.7 nM for the sigma-1 receptor and approximately 10 times selectivity over the sigma-2 receptor. Unlike its enantiomer, BD1031, BD1018 acts as a sigma receptor antagonist. Consistent with other reported sigma receptor antagonists, BD1018 decreases the behavioural toxicity of cocaine in Swiss Webster mice. See also * BD1008 * BD1031 BD1031 or (R)-2- -(3,4-dichlorophenyl)ethylctahydropyrrolo ,2-ayrazine is a selective sigma receptor agonist, with a reported binding affinity of ''K''i = 1 ± 0.2 nM for the sigma-1 receptor and 80 times selectivity over the sigma-2 receptor. Th ... References {{reflist Ligands (biochemistry) ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sigma Receptor
Sigma receptors (σ-receptors) are protein cell surface receptors that bind ligands such as 4-PPBP (4-phenyl-1-(4-phenylbutyl) piperidine), SA 4503 (cutamesine), ditolylguanidine, dimethyltryptamine, and siramesine. There are two subtypes, sigma-1 receptors (σ1) and sigma-2 receptors (σ2), which are classified as sigma receptors for their pharmacological similarities, even though they are evolutionarily unrelated. The fungal protein ERG2, a C-8 sterol isomerase, falls into the same protein family as sigma-1. Both localize to the ER membrane, although sigma-1 is also reported to be a cell surface receptor. Sigma-2 is an EXPREA domain protein (citation needed) with a mostly intracellular (ER membrane) localization. Classification Because the σ-receptor was originally discovered to be agonized by benzomorphan opioids and antagonized by naltrexone, σ-receptors were originally believed to be a type of opioid receptor. When the σ1 receptor was isolated and cloned, it was ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BD1008
BD1008 or N- -(3,4-dichlorophenyl)ethylN-methyl-1-pyrrolidineethanamine is a selective sigma receptor antagonist, with a reported binding affinity of ''K''i = 2 ± 1 nM for the sigma-1 receptor and 4 times selectivity over the sigma-2 receptor. Consistent with other reported sigma receptor Sigma receptors (σ-receptors) are protein cell surface receptors that bind ligands such as 4-PPBP (4-phenyl-1-(4-phenylbutyl) piperidine), SA 4503 (cutamesine), ditolylguanidine, dimethyltryptamine, and siramesine. There are two subtypes, ... antagonists, pretreating Swiss Webster mice with BD1008 significantly attenuates the behavioral toxicity of cocaine, and may be potentially useful in the development of antidotes for the treatment of cocaine overdose. See also * BD1031 * LR132 References {{Sigma receptor modulators Pyrrolidines Chloroarenes ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Types of agonists can be activated by either endogenous agonists (such as |
Binding Affinity
In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a molecule which produces a signal by binding to a site on a target protein. The binding typically results in a change of conformational isomerism (conformation) of the target protein. In DNA-ligand binding studies, the ligand can be a small molecule, ion, or protein which binds to the DNA double helix. The relationship between ligand and binding partner is a function of charge, hydrophobicity, and molecular structure. Binding occurs by intermolecular forces, such as ionic bonds, hydrogen bonds and Van der Waals forces. The association or docking is actually reversible through dissociation. Measurably irreversible covalent bonding between a ligand and target molecule is atypical in biological systems. In contrast to the definition of ligan ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sigma-1 Receptor
The sigma-1 receptor (σ1R), one of two sigma receptor subtypes, is a chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling through the IP3 receptor. In humans, the σ1 receptor is encoded by the ''SIGMAR1'' gene. The σ1 receptor is a transmembrane protein expressed in many different tissue types. It is particularly concentrated in certain regions of the central nervous system. It has been implicated in several phenomena, including cardiovascular function, schizophrenia, clinical depression, the effects of cocaine abuse, and cancer. Much is known about the binding affinity of hundreds of synthetic compounds to the σ1 receptor. An endogenous ligand for the σ1 receptor has yet to be conclusively identified, but tryptaminergic trace amines and neuroactive steroids have been found to activate the receptor. Especially progesterone, but also testosterone, pregnenolone sulfate, and dehydroepiandrosterone sulfate (DHEA-S) bind to the σ1 receptor. C ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sigma-2 Receptor
The sigma-2 receptor (σ2R) is a sigma receptor subtype that has attracted attention due to its involvement in diseases such as cancer and neurological diseases. It is currently under investigation for its potential diagnostic and therapeutic uses. Although the sigma-2 receptor was identified as a separate pharmacological entity from the sigma-1 receptor in 1990, the gene that codes for the receptor was identified as TMEM97 only in 2017. TMEM97 was shown to regulate the cholesterol transporter NPC1 and to be involved in cholesterol homeostasis. The sigma-2 receptor is a four-pass transmembrane protein located in the endoplasmic reticulum. It has been found to play a role in both hormone signaling and calcium signaling, in neuronal signaling, in cell proliferation and death, and in binding of antipsychotics. Classification The sigma-2 receptor is located in the lipid raft. The sigma-2 receptor is found in several areas of the brain, including high densities in the cerebellum, m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
