140850-73-3
Chemical Structure
Igmesine
Synonym(s): JO 1784
- CAS No.: 140850-73-3
- Formula:C23H29N
- Molecular Weight:319.49
IUPAC Name: (E)-N-(cyclopropylmethyl)-N-methyl-3,6-diphenylhex-5-en-3-amine
InChIKey: VCZSWYIFCKGTJI-JLHYYAGUSA-N
SMILES: C(N(CC1CC1)C)(C/C=C/C2=CC=CC=C2)(CC)C3=CC=CC=C3
Biological Activity: Igmesine (JO 1784) is a selective σ-1 receptor agonist (IC50 = 39 nM) with oral activity and blood-brain barrier penetration. Igmesine stimulates duodenal bicarbonate secretion in rats via a σ1/vagal/CCK-A-dependent pathway, without antisecretory activity. Igmesine centrally blocks CRF-mediated gastrin-inhibitory effects, and in TMT toxicity and MCAO focal ischemia models, it downregulates PTBBS, reduces NOS, and modulates M1/M2 density. Igmesine is used in research on duodenal ulcers, Alzheimer's disease, and related diseases[1][2][3][4][5][6].
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Igmesine | Igmesine (JO 1784) is a selective σ-1 receptor agonist (IC50 = 39 nM) with oral activity and blood-brain barrier penetration. Igmesine stimulates duodenal bicarbonate secretion in rats via a σ1/vagal/CCK-A-dependent pathway, without antisecretory activity. Igmesine centrally blocks CRF-mediated gastrin-inhibitory effects, and in TMT toxicity and MCAO focal ischemia models, it downregulates PTBBS, reduces NOS, and modulates M1/M2 density. Igmesine is used in research on duodenal ulcers, Alzheimer's disease, and related diseases. | |||||||||||||||||||||
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References
- [1]. Gué M, et al. Central neuropeptide Y and the sigma ligand, JO 1784, reverse corticotropin-releasing factor-induced inhibition of gastric acid secretion in rats. British journal of pharmacology. 1992 Nov;107(3):642-7.
- [2]. Pascaud XB, et al. Effects of a new sigma ligand, JO 1784, on cysteamine ulcers and duodenal alkaline secretion in rats. Gastroenterology. 1993 Feb;104(2):427-34. [Content Brief]
- [3]. Freyssin A, et al. Fluoroethylnormemantine (FENM) shows synergistic protection in combination with a sigma-1 receptor agonist in a mouse model of Alzheimer's disease. Neuropharmacology. 2024 Jan 01;242:109733.
- [4]. Roman FJ, et al. JO 1784, a potent and selective ligand for rat and mouse brain sigma-sites. The Journal of pharmacy and pharmacology. 1990 Jun;42(6):439-40. [Content Brief]
- [5]. Earley B, et al. The effects of MK-801, ifenprodil, JO 1784, JO 1994 and JO 1997 on PK 11195 receptor binding, nitric oxide synthase (NO synthase) activity and infarct volume in a mouse model of focal cerebral ischaemia. Neurochem Int. 1996 May-Jun;28(5-6):509-21.
- [6]. Earley B, et al. Effects of JO 1784, a selective sigma ligand, on the autoradiographic localization of M1 and M2 muscarinic receptor subtypes in trimethyltin treated rats. Neurochem Int. 1995 Jun;26(6):559-70.
