Sigma-1 Receptor - Ligands

Ligands

Today, ligands are known which have high affinity for the σ1 receptor and possess high binding selectivity over the subtype σ2:

• 4-IPBS
• NE-100
• L-687,384
• PD 144418
• PRE-084: agonist
• SA-4503
• spipethiane
• fluvoxamine
• RHL-033
• S1RA
• 3--4-piperidyl]methyl]-1,3-benzoxazol-2-one: very high affinity and subtype selectivity
• 1'-spiro
• 1-benzyl-6′-methoxy-6′,7′-dihydrospiropyran]: putative antagonist, selective against 5-HT_1A, 5-HT₆, 5-HT₇, α1A and α2 adrenergic, and NMDA receptors
• 1'-benzyl-6-methoxy-1-phenyl-spiropyrazole-4,4'-piperidine]
• (−)-(S)-4-methyl-1-piperidine

Agents exist that have high σ1 affinity but either lack subtype selectivity or have high affinity at other binding sites, thus being more or less dirty/multifunctional, like haloperidol. Furthermore, there is a wide range of agents with an at least moderate σ1 involvement in their binding profile.