Guanfacine
Title: Guanfacine
CAS Registry Number: 29110-47-2
CAS Name: N-(Aminoiminomethyl)-2,6-dichlorobenzeneacetamide
Additional Names: N-amidino-2-(2,6-dichlorophenyl)acetamide; [(2,6-dichlorophenyl)acetyl]guanidine
Molecular Formula: C9H9Cl2N3O
Molecular Weight: 246.09
Percent Composition: C 43.93%, H 3.69%, Cl 28.81%, N 17.08%, O 6.50%
Literature References: Centrally acting a2-adrenoceptor agonist. Prepn: J. B. Bream, C. W. Picard, FR 1584670; eidem, US 3632645 (1969, 1972, both to Wander). Pharmacology: D. M. Coward et al., Arzneim.-Forsch. 27, 2326 (1977); H. F. Oates et al., Arch. Int. Pharmacodyn. Ther. 231, 148 (1978); eidem, Clin. Exp. Pharmacol. Physiol. 6, 61 (1979). Determn in biological fluids: M. Guerrat et al., J. Pharm. Sci. 68, 219 (1979). Kinetics: Y. A. Weiss et al., Clin. Pharmacol. Ther. 25, 283 (1979). Clinical studies: U. C. Dubach et al., Arzneim.-Forsch. 27, 674 (1977); P. MacCarthy et al., Clin. Exp. Pharmacol. Physiol. 5, 187 (1978). Symposium on pharmacology, pharmacokinetics, clinical efficacy and comparison with clonidine: Am. J. Cardiol. 57, 1E-61E (1986). Review: Br. J. Clin. Pharmacol. 10, Suppl. 1, 1S-208S (1980).
Properties: White grains from methanol/ether, mp 225-227°.
Melting point: mp 225-227°
 
Derivative Type: Hydrochloride
CAS Registry Number: 29110-48-3
Manufacturers' Codes: BS-100-141; LON-798
Trademarks: Estulic (Novartis); Tenex (ESP)
Molecular Formula: C9H9Cl2N3O.HCl
Molecular Weight: 282.55
Percent Composition: C 38.26%, H 3.57%, Cl 37.64%, N 14.87%, O 5.66%
Properties: White needles, mp 213-216°. LD50 in mice: 165 mg/kg orally (Coward).
Melting point: mp 213-216°
Toxicity data: LD50 in mice: 165 mg/kg orally (Coward)
 
Therap-Cat: Antihypertensive.
Keywords: a-Adrenergic Agonist; Antihypertensive; Guanidine Derivatives.

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