Table 1.

A Selection of Common SigmaR1 Ligands.

Compound Name	Function	Clinical Use	References
Chloroquine		Anti-malarial drug	[45]
BD1047	Antagonist	Has antipsychotic properties, potential use as a neuropathic pain treatment (in phase II clinical trials)	[46,47]
BD1063	Antagonist	Reduces effects of cocaine, MDMA	[46,47]
Cannabidiol (CBD)	Antagonist	Treatment for pain, cancer symptoms and holds potential for Alzheimer’s, Parkinson’s, stroke, epilepsy, neuropsychiatric disorders	[48]
E52862	Antagonist	Potential treatment for neuropathic pain	[49]
Dehydroepiandrosterone	Agonist	Anti-aging therapy, used to treat depression and menopause symptoms	[50]
Haloperidol	Antagonist	Antipsychotic	[24]
NE-100	Antagonist	Commonly used to study SigmaR1	[51]
Progesterone	Antagonist	Important hormone of the menstrual cycle and helping maintain the early stages of pregnancy	[45,52]
Sertraline	Antagonist	Selective serotonin reuptake inhibitor used to treat depression, OCD, PTSD, and panic attacks	[53]
Verapamil	Antagonist	treats cardiac issues including angina, heart rhythm problems, and hypertension	[54]
Cocaine	Agonist	Central nervous system (CNS) stimulant	[11,12,34,55]
Choline	Agonist	Triggers IP3-evoked Ca2+ release	[56]
Donepezil	Agonist	Dementia medication	[57,58]
Dextromethorphan	Agonist	Cough suppressant	[59]
N, N-dimethyltryptamine (DMT)	Agonist	hallucinogen	[60]
Fluvoxamine	Agonist	Selective serotonin reuptake inhibitor used to treat depression and OCD	[61]
Ifenprodil	Agonist	Cerebral vasodilator	[62]
Memantine	Agonist	Used to treat Alzheimer’s disease symptoms	[47]
Methamphetamine	Agonist	Central nervous system (CNS) stimulant	[45]
Pentazocine	Agonist	Opioid pain medication	[63]
SA4503 (Cutamesine)	Agonist	Anti-amnesia properties, inhibits angiotensin II-induces cardiomyocyte hypertrophy	[64]
SKF10,47	Agonist	Opioid analgesic	[65]
4-(N-benzylpiperidin-4-yl)-4-iodobenzamide (4-IBP)	Agonist	Decreases migration of human cancer cells in vitro	[36]