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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 EXPERA domain protein [4] with a mostly intracellular (ER membrane) localization. [5]
The σ 1 receptor is defined by its unique pharmacological profile. In 1976 Martin reported that the effects of N-allylnormetazocine (SKF-10,047) could not be due to activity at the μ and κ receptors (named from the first letter of their selective ligands morphine and ketazocine, respectively) and a new type of opioid receptor was proposed; σ (from the first letter of SKF-10,047). [13]
MS-377 acts selectively at the sigma-1 receptor as an antagonist. It does not act on dopamine or serotonin receptors unlike most anti-psychotics.Tests have shown that MS-377 could displace ligand binding from the sigma-1 receptor, but did this not happen at the sigma-2, 5-HT 2 and D 2 receptors, suggesting that it is selective for the sigma-1 receptor.
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BD-1047 is a sigma receptor antagonist, selective for the σ 1 subtype. It has effects in animal studies suggestive of antipsychotic activity and may also be useful in the treatment of neuropathic pain.
BD1052 or N-[2-(3,4-dichlorophenyl)ethyl]-N-2-propen-1-yl-1-pyrrolidineethanamine is a selective sigma receptor agonist, with a reported binding affinity of K i = 2 ± 0.5 nM for the sigma-1 receptor and 30 times selectivity over the sigma-2 receptor.
Siramesine (or Lu 28-179) is a sigma receptor agonist, selective for the σ2 subtype. [1] In animal studies , siramesine has been shown to produce anxiolytic [ 2 ] and antidepressant [ 3 ] effects.
Ligands of the sigma receptor. Subcategories. This category has the following 2 subcategories, out of 2 total. S. Sigma agonists (59 P) Sigma antagonists (13 P)