ARC 239 dihydrochloride

ARC 239 dihydrochloride Property

storage temp. 

Store at RT

solubility 

<48.04mg/ml in H2O

form 

solid

color 

White

Water Solubility 

Soluble to 100 mM in water

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H400Very toxic to aquatic life

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P273Avoid release to the environment.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P391Collect spillage. Hazardous to the aquatic environment

P501Dispose of contents/container to..…

ARC 239 dihydrochloride Chemical Properties,Usage,Production

Uses

ARC 239 Dihydrochloride is a norepinephrine-serotonin reuptake inhibitor that can be used for treatment of vasomotor symptoms. ARC 239 Dihydrochloride is also an α2-adrenoceptor antagonist.

Biological Activity

arc 239 dihydrochloride is a selective antagonist of α2b adrenoceptor with pkd value of 8.8 [1].α2b adrenoceptor is a g-protein coupled receptor. α2-adrenergic receptors include three subtypes: α2a, α2b and α2c, which play an important role in regulating neurotransmitter release from adrenergic neurons in the central nervous system and from sympathetic nerves.arc 239 dihydrochloride is a selective α2b adrenoceptor antagonist. in rat brain, arc 239 inhibited the binding of 5-htia receptor radioligands 8-oh-dpat and rx 821002 to cortical membranes with ki values of 63.1 and 136 nm respectively, which suggested that arc 239 recognized 5-ht1a receptor [2]. treatment human platelets with arc 239 significantly inhibited platelet aggregation induced by adenosine diphosphate (adp), epinephrine and arachidonic acid and increased collagen/epinephrine closure time, which suggested that α2b adrenoceptor play a critical role in platelet aggregation [3]. in cervical samples isolated from pregnant rats, arc 239 effectively inhibited noradrenaline-stimulated contractions [4].in c57bl/6 mice with gastric mucosal damage induced by acidified ethanol, arc 239 (10.4 nm) antagonized gastroprotective effect induced by α2-adrenoceptor agonists [5].

IC 50

Alpha-2B adrenergic receptor; 5-HT_1A Receptor

storage

Store at RT

References

[1]. bylund db, ray-prenger c, murphy tj. alpha-2a and alpha-2b adrenergic receptor subtypes: antagonist binding in tissues and cell lines containing only one subtype. j pharmacol exp ther, 1988, 245(2): 600-607.
[2]. meana jj, callado lf, pazos a, et al. the subtype-selective alpha 2-adrenoceptor antagonists brl 44408 and arc 239 also recognize 5-ht1a receptors in the rat brain. eur j pharmacol, 1996, 312(3): 385-388.
[3]. marketou me, kintsurashvili e, androulakis ne, et al. blockade of platelet alpha2b-adrenergic receptors: a novel antiaggregant mechanism. int j cardiol, 2013, 168(3): 2561-2566.
[4]. gál a, kolarovszki-sipiczki z, et al. the effect of the arc 239 on the myometrial and cervical action in the rat, in vitro. acta pharm hung, 2009, 79(2): 75-80.
[5]. zádori zs, shujaa n, brancati sb, et al. both α2b- and α2c-adrenoceptor subtypes are involved in the mediation of centrally induced gastroprotection in mice. eur j pharmacol, 2011, 669(1-3): 115-120.