85409-38-7

85409-38-7 structure

Name: Rilmenidine phosphate
Chemical Name: N-(dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine,phosphoric acid
CAS Number: 85409-38-7
Molecular Formula: C₁₀H₁₉N₂O₅P
Molecular Weight: 278.242
Catalog: analytical chemistry Standard Pharmacopoeia Standards and Magazine Standards
Create Date: 2018-08-24 19:57:50
Modify Date: 2024-01-02 09:23:33
Rilmenidine phosphate, an antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate is also an alpha 2-adrenoceptor agonist. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].

Name	N-(dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine,phosphoric acid
Synonyms	2-Oxazolamine, N-(dicyclopropylmethyl)-4,5-dihydro-, phosphate (1:1) N-(Dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine phosphate (1:1) Rilmenidine phosphate 2-Oxazolamine, 4,5-dihydro-N-(dicyclopropylmethyl)-, phosphate (1:1) S 3341-3 {Phosphate} Rilmenidine dihydrogen phosphate S 3341-3 EINECS 287-106-2 4,5-Dihydro-N-(dicyclopropylmethyl)-2-oxazolamine phosphate (1:1) Hyperium

Description	Rilmenidine phosphate, an antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate is also an alpha 2-adrenoceptor agonist. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> Imidazoline Receptor Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cardiovascular Disease Signaling Pathways >> GPCR/G Protein >> Imidazoline Receptor Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
In Vitro	Rilmenidine phosphate (25-100 μM; 24 hours) inhibits K562 cell proliferation[2].Rilmenidine provides antihypertensive efficacy comparable with that of diuretics, beta-blockers, calcium channel blockers, and angiotensin-converting enzyme (ACE) inhibitors[3]. Cell Proliferation Assay[2] Cell Line: K562 cells Concentration: 25, 50, 100 μM Incubation Time: 24 hours Result: Dose-dependently inhibited K562 colony formation.
In Vivo	Rilmenidine phosphate-treated N171-82Q mice (i.p.; 4-times a week) displays significant improved forelimb grip strength and all limbs grip strength from 12 to 22 weeks of age[4]. Rilmenidine phosphate decreases levels of mutant huntingtin[4].
References	[1]. Reid JL. Rilmenidine: a clinical overview. Am J Hypertens. 2000;13(6 Pt 2):106S-111S. [2]. Srdic-Rajic T, et al. Rilmenidine suppresses proliferation and promotes apoptosis via the mitochondrial pathway in human leukemic K562 cells. Eur J Pharm Sci. 2016;81:172-180. [3]. Reid JL. Rilmenidine: a clinical overview. Am J Hypertens. 2000;13(6 Pt 2):106S-111S. [4]. Rose C, et al. Rilmenidine attenuates toxicity of polyglutamine expansions in a mouse model of Huntington's disease. Hum Mol Genet. 2010;19(11):2144-2153.

Boiling Point	609.1ºC at 760 mmHg
Molecular Formula	C₁₀H₁₉N₂O₅P
Molecular Weight	278.242
Flash Point	322.1ºC
Exact Mass	278.103149
PSA	121.19000
LogP	0.04870
Storage condition	-20℃
Water Solubility	Freely soluble in water, slightly soluble in alcohol, practically insoluble in methylene chloride.

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RP6744000

CAS REGISTRY NUMBER :: 85409-38-7

LAST UPDATED :: 199512

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C10-H16-N2-O.H3-O4-P

MOLECULAR WEIGHT :: 278.28

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 295 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,56,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 375 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 8,56,1990

HS Code	2934999090

HS Code	2934999090
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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