Cutamesine - CAS 165377-43-5
Catalog number: 165377-43-5
Category: Inhibitor
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Molecular Formula:
C23H32N2O2
Molecular Weight:
368.51
COA:
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Targets:
Sigma Receptor
Description:
Cutamesine, also called as SA4503, is an agonist, small-molecule ligand for the sigma-1 receptor with high selectivity currently in development to mediate neuroprotection and regeneration in the context of neurodegenerative disease. in vitro: reduced SOD1
Appearance:
Solid powder
Synonyms:
1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazine (11C)SA4503 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine dihydrochloride cutamesine SA 4503 SA-4503 SA4503
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -58℃ for long term (months to years).
MSDS:
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Shelf Life:
2 years
Quantity:
Grams-Kilos
Boiling Point:
499.2±45.0 °C | Condition: Press: 760 Torr
Density:
1.053±0.06 g/cm3
InChIKey:
UVSWWUWQVAQPJR-UHFFFAOYSA-N
InChI:
1S/C23H32N2O2/c1-26-22-11-10-21(19-23(22)27-2)12-14-25-17-15-24(16-18-25)13-6-9-20-7-4-3-5-8-20/h3-5,7-8,10-11,19H,6,9,12-18H2,1-2H3
Canonical SMILES:
COC1=C(C=C(C=C1)CCN2CCN(CC2)CCCC3=CC=CC=C3)OC
1.Sertoli cell line lacks the immunoprotective properties associated with primary Sertoli cells.
Dufour JM;Dass B;Halley KR;Korbutt GS;Dixon DE;Rajotte RV Cell Transplant. 2008;17(5):525-34.
Sertoli cells are important for maintenance of the immune privileged environment of the testis and prolong survival of cotransplanted cells. The objective of the current study was to examine the immunoprotective properties of a mouse Sertoli cell line (MSC-1) in order to identify a Sertoli cell line that could be used to aid in investigation of the immunoprotective abilities of Sertoli cells. BALB/c islets were cotransplanted with 0-9 million primary BALB/c Sertoli cells or MSC-1 cells into diabetic C3H or BALB/c mice and protection of grafted islets was examined by monitoring blood glucose levels and immunohistochemical analysis. Additionally, expression of potential immunoprotective factors in MSC-1 cells was examined. Cotransplantation of islets with 3 million primary Sertoli cells significantly prolonged islet allograft survival (61.1 +/- 6.9 days; p < 0.05) compared with control mice that received allogeneic islets alone (26.9 +/- 2.1 days). Grafts collected from normoglycemic C3H mice at 100 days posttransplant contained insulin-positive beta-cells adjacent to allogeneic Sertoli cells arranged in tubule-like structures. In contrast, cotransplantation of islet allografts with MSC-1 cells did not prolong islet survival (average 29.
2.Evaluation of (+)-p-[11C]methylvesamicol for mapping sigma1 receptors: a comparison with [11C]SA4503.
Ishiwata K;Kawamura K;Yajima K;QingGeLeTu;Mori H;Shiba K Nucl Med Biol. 2006 May;33(4):543-8. Epub 2006 May 3.
Vesamicol is a leading compound for positron emission tomography (PET) and single photon emission computed tomography (SPECT) tracers for mapping the vesicular acetylcholine transporter (VAChT). Recently, we found that (+)-p-methylvesamicol ((+)-PMV) has low affinity for VAChT (K(i)=199 nM), but has moderate to high affinity for sigma receptors: K(i)=3.0 nM for sigma1 and K(i)=40.7 nM for sigma2, and that sigma1-selective SA4503 (K(i)=4.4 nM for sigma1 and K(i)=242 nM for sigma2) has moderate affinity for VAChT (K(i)=50.2 nM). In the present study, we examined the potential of (+)-[11C]PMV as a PET radioligand for mapping sigma1 receptors as compared with [11C]SA4503. In rat brain, similar regional distribution patterns of (+)-[11C]PMV and [11C]SA4503 were shown by tissue dissection and by ex vivo autoradiography. Blocking experiments using (+/-)-PMV, (-)-vesamicol, SA4503, haloperidol and (+/-)-pentazocine showed that the two tracers specifically bound to sigma1 receptors, and that [11C]SA4503 exhibited greater specific binding than (+)-[11C]PMV. No sign of VAChT-specific binding by [11C]SA4503 was observed in the striatum, which is rich in VAChT sites. In conclusion, (+)-[11C]PMV specifically bound to sigma1 receptors in the brain, but to a lesser extent than [11C]SA4503, suggesting that (+)-[11C]PMV is a less preferable PET ligand than [11C]SA4503.
3.Age-related changes of the binding of [3h]SA4503 to sigma1 receptors in the rat brain.
Ishiwata K;Kobayashi T;Kawamura K;Matsuno K Ann Nucl Med. 2003 Feb;17(1):73-7.
We have recently developed 1-([3-O-methyl-11C]3,4-dimethoxyphenethyl)-4-(3-phenylpropyl) piperazine ([11C]SA4503) as a selective radioligand for mapping sigma1 receptors in the brain by positron emission tomography (PET). In the present short communication we evaluated the age-related changes of the binding of this ligand to sigma1 receptors in Fisher-344 rats (1.5-, 6-, 12-, and 24-month-old) by the in vitro binding assay. We also measured the binding of [3H](+)-pentazocine to sigma1 receptors and the binding of [3H]1,3-di-O-tolylguanidine to sigma2 receptors, which are current standard methods. The specific binding of the three radioligands increased age-dependently. Both Kd and Bmax values of the 24-month-old rats for each radioligand were significantly higher than those of the young rats (1.5- and 6-month-old). The increased numbers of both sigma1 and sigma2 receptor subtypes in the aged rats compensate for the lowered affinity, and rather enhanced the radioligand-receptor binding. The results contrast strikingly with the age-dependent decrease in the dopaminergic, cholinergic and glutamatergic receptors that are reported to be correlated with the sigma receptors, and indicate that a PET study with [11C]SA4503 to evaluate the aging process in humans would be of great interest.
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CAS 165377-43-5 Cutamesine

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