|Description||The sigma-1 (σ1) receptor is an intracellular, non-opioid receptor that is abundantly expressed in the central nervous system as well as peripherally. S1RA is a potent, selective antagonist of σ1 receptors (Ki = 17 nM) that weakly binds σ2 receptors (Ki = 9,300 nM).|
BD 1008 dihydrobromide
BD 1008 dihydrobromide is a potent and selective σ receptor antagonist displaying 4-fold selectivity for σ1 over σ2. BD-1008 attenuates the toxicity and stimula...
N-[2-(Piperidinylamino)ethyl]-4-iodobenzamide is a selective ligand belongs to benzamides, therapeutic agents for human prostate tumors sigma-1, which binds wit...
BD1063 dhydrochloride is a potent and selective antagonist of sigma 1 receptor(Ki= 9.15 nM)with 50-fold more selective over sigma-2(Ki= 449 nM) and >100-fold mo...
4-IBP, an agonist that specially targets sigma receptor (IC50= 1.7 nM), induced marked concentration-dependent decreases in the growth of human cancer cells. σ1...
MIN-101, a novel cyclic amide derivative, is a 5-HT2A and sigma 2 receptor antagonist (Ki= 7.53 nM for 5-HT2A and 8.19 nM for sigma-2, respectively).
Sigma-LIGAND-1, also called as NPC 16377, is a selective sigma receptor ligand developed for the treatment of neurological disorders and psychotic disorders in ...
Siramesine is a selective sigma-2 receptor agonist with a potent anticancer activity in vivo. It was originally devevloped for treating depressant and it has pr...
PB 28 dihydrochloride
PB 28 dihydrochloride is a high affinity σ2 receptor agonist. It displays antiproliferative and cytotoxic effects in SK-N-SH neuroblastoma and C6 glioma cells.
DTG has been found to be a σ-receptor agonist and is useful in studies of its interaction with dopamine drug.
L-693,403 maleate is the maleate salt of L-693,403, which is a sigma receptor-binding compound. It has excellent selectivity over the dopamine D2 receptor and b...
4-PPBP, a piperidine derivative, is a σ ligand and selective non-competitive antagonist at recombinant NR1a/2B NMDA receptors expressed in Xenopus oocytes. It i...
Noscapine is a phthalideisoquinoline alkaloid derived from the opium poppy Papaver somniferum, with mild analgesic, antitussive, and potential antineoplastic ac...
The hydrochloride salt form of S1RA which is a σ1 receptor antagonist that has been found to have potential effect in pain therapy. It is still under Phase II c...
SM-21 maleate is a potent and selective σ2 antagonist that can increase acetylcholine release at central muscarinic synapses. SM-21 is used as a potent analgesi...
BMY 14802 hydrochloride
BMY 14802 hydrochloride is a potent sigma receptor antagonist (IC50 = 112 nM) with weak affinity for 5-HT1A and α1 receptors. BMY 14802 is potentially used as a...
BD 1047 dihydrobromide
The dihydrobromide salt form of BD-1047, a selective σ1 receptor antagonist, has been found to have antipsychotic effect and could be probably used against schi...
Rimcazole dihydrochloride is a small molecule antagonist of the σ-1 receptor (IC50 values are 1480 and 386 nM at σ1 and σ2 receptors respectively).
TC 1 is a high affinity σ1 receptor ligand with selectivity over σ2 receptors (Ki = 10 and 370 nM respectively). TC 1 exhibits low affinity for dopamine (DAT), ...
PRE-084 hydrochloride is a high affinity, selective receptors exhibiting neuroprotective effects. Its IC50 value is 44 nM in the sigma receptor assay. In vitro,...
(±)-PPCC oxalate is a selective sigma (σ) receptor ligand, which is noted to exhibit high affinity for σ1 and also binds at σ2 sites (Ki = 1.5 nM and 50.8 nM re...