SIGMAR1 binds fluvoxamine

Stable Identifier
R-HSA-9679780
Type
Reaction [binding]
Species
Homo sapiens
Compartment
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Among selective serotonin reuptake inhibitors (SSRIs), fluvoxamine shows high affinity for sigma-1 receptors (SIGMAR1). Binding (Ishikawa et al. 2007) and stimulation of SIGMAR1 by fluvoxamine elicits antipdepressive effects in rats (Yagasaki et al. 2006, Fishback et al. 2010). The endogenous ligand for SIGMAR1 may be progesterone (Ganapathy et al. 1999). Small anecdotal studies suggest that ligands that target SIGMAR1 may be useful in treating central hypoventilation syndromes (Loiseau et al. 2018), suggesting a possible role for such drugs in treatment of COVID-19 symptoms.

Literature References
PubMed ID Title Journal Year
23641311 From α4β2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design

Yu, LF, Zhang, HK, Gunosewoyo, H, Kozikowski, AP

ACS Med Chem Lett 2012
16522641 Chronic antidepressants potentiate via sigma-1 receptors the brain-derived neurotrophic factor-induced signaling for glutamate release

Yagasaki, Y, Numakawa, T, Kumamaru, E, Hayashi, T, Su, TP, Kunugi, H

J. Biol. Chem. 2006
17662961 High occupancy of sigma-1 receptors in the human brain after single oral administration of fluvoxamine: a positron emission tomography study using [11C]SA4503

Ishikawa, M, Ishiwata, K, Ishii, K, Kimura, Y, Sakata, M, Naganawa, M, Oda, K, Miyatake, R, Fujisaki, M, Shimizu, E, Shirayama, Y, Iyo, M, Hashimoto, K

Biol. Psychiatry 2007
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