PRE-084
- Product Name
- PRE-084
- CAS No.
- 75136-54-8
- Chemical Name
- PRE-084
- Synonyms
- PRE-084 hydrochloride ，S6950;PRE-084 hydrochloride, 10 mM in DMSO;2-morpholinoethyl 1-phenylcyclohexane-1-carboxylate hydrochloride;1-Phenylcyclohexanecarboxylic acid 2-(4-morpholinyl)ethyl ester hydrochloride
- CBNumber
- CB3498338
- Molecular Formula
- C19H28ClNO3
- Formula Weight
- 353.88352
- MOL File
- 75136-54-8.mol
PRE-084 Property
- storage temp.
- Store at RT
- solubility
- H2O: ≤24 mg/mL
- form
- solid
- color
- White to off-white
- Stability:
- Hygroscopic
Safety
- WGK Germany
- 3
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 9001329
- Product name
- PRE-084 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $96
- Updated
- 2024/03/01
- Product number
- 9001329
- Product name
- PRE-084 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $427
- Updated
- 2024/03/01
- Product number
- 9001329
- Product name
- PRE-084 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 100mg
- Price
- $758
- Updated
- 2024/03/01
- Product number
- M725060
- Product name
- 2-(4-Morpholinyl)ethyl1-PhenylcyclohexaneCarboxylateHydrochloride
- Packaging
- 100mg
- Price
- $180
- Updated
- 2021/12/16
- Product number
- CS-5241
- Product name
- PRE-084hydrochloride
- Purity
- 99.80%
- Packaging
- 200mg
- Price
- $990
- Updated
- 2021/12/16
PRE-084 Chemical Properties,Usage,Production
Uses
2-(4-Morpholinyl)ethyl 1-Phenylcyclohexane Carboxylate Hydrochloride is a selective sigma-1 receptor agonist exhibiting neuroprotective effects.
Biological Activity
ki: 2.2 and 13091 nm for σ1 and σ2 receptors respectively.pre-084 hydrochloride is a selective σ1 agonist with high affinity, rather than over pcp receptors (ic50 > 100000 nm) and several other receptor systems. it was reported that sigma (s) receptor ligands to alleviate learning and memory impairments on several pharmacological and pathological rodent models of amnesia, involving the s1 subtype of s receptor.
in vitro
pre-084 had an ic50 of 44 nm in the receptor assay and an ic50 of more than 100,000 nm for pcp receptors and an ic50 higher than 1 0,000 nm in many other receptor systems. in general, hydroxy-substituted phenyl groups in these compounds like pre-084 tended to have attenuated potency at a receptors, whereas methylphenyl and chlorophenyl substitutions enhanced potencies. reduction of cycloalkyl ring size lowered potencies for a receptors and quatemized amine groups invariably decreased the compound’s potencies. [1]. the sig-1r agonist pre084 not only increases cell survival, but also counteracts the deleterious effects caused by nmhp in neuronal pc6.3 cells. particularly, pre084 stimulates the nf-kb pathway that is compromised by the expression of mutant huntingtin proteins, increasing the levels of cellular antioxidants. these data show that the sig-1r agonist beneficially effects on models of hd and that compounds binding the sig-1r may be potent targets for future drug development in hd [2].
in vivo
after exposure to co or 14 days after intoxication with trimethyltin, the spontaneous alternation deficits was reversed significantly by the selective sigma1 ligand pre-084 (1 mg kg-1) [3]. administration of pre-084 (5 mg/kg, i.p.) inhibited citric-acid-induced cough in guinea-pigs. in addition, when administered by aerosol, sigma agonist pre-084 (1 mg/ml) inhibited cough [4].
IC 50
eNOS; Sigma 1 Receptor
References
[1]. su tp, wu xz, cone ej, shukla k, gund tm, dodge al, parish dw. sigma compounds derived from phencyclidine: identification of pre-084, a new, selective sigma ligand. j pharmacol exp ther. 1991 nov;259(2):543-50.
[2]. hyrskyluoto a, pulli i, trnqvist k, ho th, korhonen l, lindholm d. sigma-1 receptor agonist pre084 is protective against mutant huntingtin-induced cell degeneration: involvement of calpastatin and the nf-κb pathway. cell death dis. 2013 may 23; 4:e646.
[3]. maurice t, phan vl, noda y, yamada k, privat a, nabeshima t. the attenuation of learning impairments induced after exposure to co or trimethyltin in mice by sigma (sigma) receptor ligands involves both sigma1 and sigma2 sites. br j pharmacol. 1999 may; 127(2):335-42.
[4]. brown c, fezoui m, selig wm, schwartz ce, ellis jl. antitussive activity of sigma-1 receptor agonists in the guinea-pig. br j pharmacol. 2004 jan; 141(2):233-40. epub 2003 dec 22.
PRE-084 Preparation Products And Raw materials
Raw materials
Preparation Products
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