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  • Rilmenidine
Name:Rilmenidine
CAS No:54187-04-1

PRODUCT DESCRIPTION

【Name】
2-Oxazolamine,N-(dicyclopropylmethyl)-4,5-dihydro-
【Iupac name】
N-(dicyclopropylmethyl)-4,5-dihydro-1,3-oxazol-2-amine
【CAS Registry number】
54187-04-1
【Synonyms】
NSC 664312
Oxaminozoline
Rilmenidene
Rilmenidine
S 3341
【EINECS(EC#)】
259-021-0
【Molecular Formula】
C10H16N2O (Products with the same molecular formula)
【Molecular Weight】
180.24684
【Inchi】
InChI=1S/C10H16N2O/c1-2-7(1)9(8-3-4-8)12-10-11-5-6-13-10/h7-9H,1-6H2,(H,11,12)
【InChIKey】
CQXADFVORZEARL-UHFFFAOYSA-N
【Canonical SMILES】
C1CC1C(C2CC2)NC3=NCCO3
【MOL File】
54187-04-1.mol

Chemical and Physical Properties

【Appearance】
solid
【Density】
1.45 g/cm3
【Melting Point】
106 - 107
【Boiling Point】
355.5 °C at 760 mmHg
【Flash Point】
168.8 °C
【Water】
H2O: 7.3 mg/mL in water
【Solubilities】
H2O: 7.3 mg/mL in water
【Color/Form】
white
【Stability】
Stable at normal temperatures and pressures.
【Storage temp】
Keep tightly closed.
【Computed Properties】
Molecular Weight:180.24684 [g/mol]
Molecular Formula:C10H16N2O
XLogP3-AA:1.2
H-Bond Donor:1
H-Bond Acceptor:2
Rotatable Bond Count:4
Tautomer Count:2
Exact Mass:180.126263
MonoIsotopic Mass:180.126263
Topological Polar Surface Area:33.6
Heavy Atom Count:13
Formal Charge:0
Complexity:219
Isotope Atom Count:0
Defined Atom Stereocenter Count:0
Undefined Atom Stereocenter Count:0
Defined Bond Stereocenter Count:0
Undefined Bond Stereocenter Count:0
Covalently-Bonded Unit Count:1
Feature 3D Donor Count:1
Feature 3D Cation Count:1
Feature 3D Ring Count:1
Effective Rotor Count:5.8
Conformer Sampling RMSD:0.6
CID Conformer Count:39

Safety and Handling

【Safety Statements 】
S22;S24/25
【Safety】

Safety Information of Rilmenidine (54187-04-1):
Safety Statements: 22-24/25  
22:  Do not breathe dust  
24/25:  Avoid contact with skin and eyes  
WGK Germany: 3
RTECS: RP7207400 
 

【Specification】

Side effects of Rilmenidine (54187-04-1):
1.At a dose of 1 mg given as a single daily administration during controlled trials, the incidence of side effects was comparable to that observed with placebo. 
2.At a dose of 2 mg per day of rilmenidine, controlled comparative studies versus clonidine (0.15 to 0.30 mg/day) or alpha2-methyldopa (500 to 1000 mg/day) demonstrated that the incidence of side effects was significantly lower with rilmenidine than with either clonidine or a-methyldopa. 
Side-effects are rare, non-severe, and transient at therapeutic doses: asthenia, palpitations, insomnia, drowsiness, fatigue on exercise, epigastric pain, dryness of the mouth, diarrhea, skin rash; and exceptionally, cold extremities, postural hypotension, sexual disorders, anxiety, depression, pruritus, edema, cramps, nausea, constipation, hot flushes

 

Use and Manufacturing

【Usage】
Selective i1 imidazoline receptor agonist.

Biomedical Effects and Toxicity

【Biological Activity】
I 1 -imidazoline binding site selective ligand and α 2 -adrenoceptor agonist. Possesses greater I 1 vs α 2 selectivity than the prototypical compound, clonidine.
【Pharmacological Action】
- Drugs that selectively bind to and activate alpha adrenergic receptors.
- Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.
【Biomedical Effects and Toxicity】
I 1 -imidazoline binding site selective ligand and α 2 -adrenoceptor agonist. Possesses greater I 1 vs α 2 selectivity than the prototypical compound, clonidine.

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