The sigma-1 receptor (σ1R), one of two sigma receptor subtypes, is a chaperone protein at the endoplasmic reticulum (ER) that modulates calcium signaling...
34 KB (3,792 words) - 16:38, 21 May 2025
Sigma receptors (σ-receptors) are protein receptors that bind ligands such as 4-PPBP (4-phenyl-1-(4-phenylbutyl) piperidine), SA 4503 (cutamesine), ditolylguanidine...
17 KB (1,832 words) - 12:09, 22 May 2025
The sigma-2 receptor (σ2R) is a sigma receptor subtype that has attracted attention due to its involvement in diseases such as neurological diseases, neurodegenerative...
22 KB (2,332 words) - 15:38, 28 April 2025
protein, the sigma-2 receptor, found in cell membranes. It is highly selective for this over the related sigma-1 receptor. The sigma-2 receptor is significant...
2 KB (216 words) - 21:23, 21 February 2025
derivative of phenylpiracetam, is a positive allosteric modulator of the sigma σ1 receptor. It is currently the only racetam known to possess this action. In...
17 KB (1,705 words) - 02:38, 22 April 2025
pregn-5-en-3β-ol-20-one 3β-sulfate – GABAA receptor negative allosteric modulator, NMDA receptor positive allosteric modulator, sigma-1 receptor agonist, TRPM3 agonist,...
19 KB (2,002 words) - 02:02, 18 May 2025
Neurosteroid (section Sigma-1 receptor)
perspective on the new mechanism of antidepressants: neuritogenesis through sigma-1 receptors". Pharmacopsychiatry. 37 (Suppl 3): S208–13. doi:10.1055/s-2004-832679...
42 KB (4,402 words) - 13:14, 30 March 2025
MS-377 (category Sigma receptor modulators)
selective antagonist of the sigma-1 receptor. It possesses anti-psychotic properties. MS-377 acts selectively at the sigma-1 receptor as an antagonist. It does...
4 KB (327 words) - 21:27, 30 March 2025
Methylphenylpiracetam (category Receptor modulators)
derivative of piracetam and a positive allosteric modulator of the sigma-1 receptor. It differs from phenylpiracetam by having a methyl group. E1R is the...
7 KB (536 words) - 18:47, 24 May 2025
Cutamesine (category Sigma agonists)
Cutamesine (SA 4503) is a synthetic sigma receptor agonist which is selective for the σ1 receptor, a chaperone protein mainly found in the endoplasmic...
14 KB (1,438 words) - 05:41, 9 April 2025
Pridopidine (category Sigma agonists)
molecule investigational drug. Pridopidine is a selective and potent Sigma-1 Receptor agonist. It is being developed by Prilenia Therapeutics and is currently...
15 KB (1,571 words) - 03:24, 23 December 2024
Diproqualone (category GABAA receptor positive allosteric modulators)
possibly its agonist activity at both the sigma-1 receptor and sigma-2 receptor (the function of these receptors and their clinical relevance has not yet...
4 KB (236 words) - 09:07, 21 January 2025
diethylamide), psilocin, and DMT. Differential 5-HT receptor affinities, as well as novel sigma-1 receptor properties, suggest potential future medicinal uses...
5 KB (376 words) - 00:30, 29 May 2025
6-tetrahydro-5-[3-(4-methylphenyl)-5-isoxazolyl]-1-propylpyridine is a potent and selective ligand for the sigma-1 receptor, with a reported binding affinity of Ki...
2 KB (96 words) - 14:55, 17 January 2025
as an antitussive. Unlike many antitussives, it binds poorly to the sigma-1 receptor. Friedel-Crafts acylation of benzene with propionyl chloride and aluminium...
5 KB (318 words) - 05:04, 10 March 2025
Cloroqualone (category GABAA receptor positive allosteric modulators)
resulting from its agonist activity at the β subtype of the GABAa receptor and sigma-1 receptor, and was sold either alone or in combination with other ingredients...
3 KB (166 words) - 15:42, 4 March 2024
as the absolute mean value. In biology, the sigma receptor (σ–receptors) is a type of cell surface receptor. In biochemistry, the σ factor (or specificity...
18 KB (2,191 words) - 13:06, 3 June 2025
emission tomography (PET) scans to image σ1 (sigma-1) receptors in the brain and other tissues. Sigma-1 receptors are proteins involved in many neurological...
6 KB (215 words) - 04:34, 23 May 2025
intracellular receptors that promote monoamine neurotransmission. For instance, methamphetamine acts as an agonist of sigma-1 receptor. ATS use disorders...
23 KB (2,404 words) - 22:09, 23 May 2025
Memantine/donepezil (category NMDA receptor antagonists)
an NMDA receptor antagonist, among various other types of targets like 5-HT3 receptor, Nicotinic acetylcholine receptor, and Sigma-1 receptor) and donepezil...
5 KB (203 words) - 21:28, 29 May 2025
Dimethyltryptamine (category Sigma agonists)
demonstrated the immunomodulatory potential of DMT and 5-MeO-DMT through the Sigma-1 receptor of human immune cells. This immunomodulatory activity may contribute...
175 KB (16,823 words) - 07:19, 3 June 2025
BD1018 (category Sigma receptor modulators)
2-a]pyrazine is a selective sigma receptor ligand, with a reported binding affinity of Ki = 5 ± 0.7 nM for the sigma-1 receptor and approximately 10 times...
2 KB (125 words) - 21:26, 30 March 2025
Opipramol (category Sigma agonists)
most other tricyclic antidepressants, and instead acts primarily as a sigma-1 receptor agonist. It was developed by Schindler and Blattner in 1961. Opipramol...
27 KB (2,047 words) - 20:11, 24 May 2025
Selective serotonin reuptake inhibitor (category Sigma receptor modulators)
gradual changes in brain signaling and receptor regulation, with some also interacting with sigma-1 receptors, particularly fluvoxamine, which may contribute...
155 KB (16,564 words) - 05:23, 1 June 2025
Sertraline (redirect from CP 51,974-1)
Hashimoto K (2017). "Sigma-1 Receptor Agonists and Their Clinical Implications in Neuropsychiatric Disorders". Sigma Receptors: Their Role in Disease...
106 KB (10,798 words) - 04:54, 5 June 2025
E-52862 (category Sigma antagonists)
E-52862, also known as sigma-1 receptor antagonist (S1A, S1RA), as well as MR-309, is a selective sigma-1 receptor antagonist, with a reported binding...
6 KB (519 words) - 16:22, 11 January 2025
achieved. In 1806, with Louis Nicolas Vauquelin), cantharidin (1810), the sigma-1 receptor agonist noscapine (1817), caffeine (1821), alizarin (later on moved...
19 KB (2,589 words) - 23:42, 27 May 2025
is the first known and published positive allosteric modulator of Sigma 1 receptor that improves memory processes and prevents seizures. Ivars KALVIŅŠ...
5 KB (305 words) - 23:11, 25 December 2024
alpha-1 (α1) adrenergic are G protein-coupled receptors (GPCRs) associated with the Gq heterotrimeric G protein. α1-adrenergic receptors are subdivided...
16 KB (1,527 words) - 14:51, 25 May 2025
Cannabinoid receptor 1 (CB1), is a G protein-coupled cannabinoid receptor that in humans is encoded by the CNR1 gene. And discovered, by determination...
42 KB (4,352 words) - 07:40, 17 May 2025