CAS 63590-64-7|Terazosin

Introduction：Basic information about CAS 63590-64-7|Terazosin, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Terazosin BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
5. Safety Information
6. Articles35
7. Synonyms

Common Name	Terazosin
CAS Number	63590-64-7	Molecular Weight	387.43300
Density	1.332 g/cm3	Boiling Point	664.5ºC at 760 mmHg
Molecular Formula	C₁₉H₂₅N₅O₄	Melting Point	281-283°C
MSDS	ChineseUSA	Flash Point	355.7ºC
Symbol	GHS07	Signal Word	Warning

Names

Name	terazosin
Synonym	More Synonyms

Terazosin BiologicalActivity

Description	Terazosin is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH).Target: Alpha-1 Adrenergic ReceptorTerazosin is selective for alpha 1A-adrenoceptors which appear to dominate in the human prostate; the therapeutic relevance of this selectivity remains to be assessed in clinical studies [1]. Administration of terazosin 1 mg orally for 28 d. Terazosin initially shifted the dose-response curve of phenylephrine to the right, with a significant increase in ED50 for phenylephrine from a control value of 102 to 759 ng/min on day 1 of terazosin (P < 0.001). The mean Kd of terazosin was estimated as 11 +/- 15 nM in the first few days of treatment. This study demonstrates that pharmacological tolerance to the alpha 1-adrenoceptor blocking action of terazosin occurs in man and may be responsible for loss in efficacy with chronic therapy [2].
Related Catalog	Signaling Pathways >>GPCR/G Protein >>Adrenergic ReceptorNatural Products >>AlkaloidResearch Areas >>Metabolic Disease
References	[1]. Michel, M.C., et al., Drugs for treatment of benign prostatic hyperplasia: affinity comparison at cloned alpha 1-adrenoceptor subtypes and in human prostate. J Auton Pharmacol, 1996. 16(1): p. 21-8. [2]. Vincent, J., et al., Pharmacological tolerance to alpha 1-adrenergic receptor antagonism mediated by terazosin in humans. J Clin Invest, 1992. 90(5): p. 1763-8.

Description

Terazosin is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH).Target: Alpha-1 Adrenergic ReceptorTerazosin is selective for alpha 1A-adrenoceptors which appear to dominate in the human prostate; the therapeutic relevance of this selectivity remains to be assessed in clinical studies [1]. Administration of terazosin 1 mg orally for 28 d. Terazosin initially shifted the dose-response curve of phenylephrine to the right, with a significant increase in ED50 for phenylephrine from a control value of 102 to 759 ng/min on day 1 of terazosin (P < 0.001). The mean Kd of terazosin was estimated as 11 +/- 15 nM in the first few days of treatment. This study demonstrates that pharmacological tolerance to the alpha 1-adrenoceptor blocking action of terazosin occurs in man and may be responsible for loss in efficacy with chronic therapy [2].

Related Catalog

Signaling Pathways >>GPCR/G Protein >>Adrenergic ReceptorNatural Products >>AlkaloidResearch Areas >>Metabolic Disease

References

[1]. Michel, M.C., et al., Drugs for treatment of benign prostatic hyperplasia: affinity comparison at cloned alpha 1-adrenoceptor subtypes and in human prostate. J Auton Pharmacol, 1996. 16(1): p. 21-8.

[2]. Vincent, J., et al., Pharmacological tolerance to alpha 1-adrenergic receptor antagonism mediated by terazosin in humans. J Clin Invest, 1992. 90(5): p. 1763-8.

Chemical & Physical Properties

Density	1.332 g/cm3
Boiling Point	664.5ºC at 760 mmHg
Melting Point	281-283°C
Molecular Formula	C₁₉H₂₅N₅O₄
Molecular Weight	387.43300
Flash Point	355.7ºC
Exact Mass	387.19100
PSA	103.04000
LogP	1.64090
InChIKey	VCKUSRYTPJJLNI-UHFFFAOYSA-N
SMILES	COc1cc2nc(N3CCN(C(=O)C4CCCO4)CC3)nc(N)c2cc1OC
Storage condition	-20°C Freezer
Water Solubility	H2O: 25 mg/mL

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TK8044925

CHEMICAL NAME :: Piperazine, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-((tetrahyd ro-2-furanyl)carbonyl )-

CAS REGISTRY NUMBER :: 63590-64-7

LAST UPDATED :: 199806

DATA ITEMS CITED :: 1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3 gm/kg

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

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4734418

Safety Information

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes	Xn: Harmful;
Risk Phrases	R22
Safety Phrases	S26
RIDADR	NONH for all modes of transport
WGK Germany	3
RTECS	TK8044925

Articles35

Noradrenergic modulation of masseter muscle activity during natural rapid eye movement sleep requires glutamatergic signalling at the trigeminal motor nucleus.

J. Physiol. 592(Pt 16) , 3597-609, (2014)

Noradrenergic neurotransmission in the brainstem is closely coupled to changes in muscle activity across the sleep-wake cycle, and noradrenaline is considered to be a key excitatory neuromodulator tha...

Method development for impurity profiling in SFC: The selection of a dissimilar set of stationary phases.

J. Pharm. Biomed. Anal. 111 , 333-43, (2015)

Supercritical fluid chromatography (SFC) is drawing considerable interest as separation technique in the pharmaceutical industry. The technique is already well established in chiral separations both a...

Efficacy of three different alpha 1-adrenergic blockers and hyoscine N-butylbromide for distal ureteral stones.

Int. Braz J Urol 37(2) , 195-200; discussion 201-2, (2011)

To evaluate hyoscine N-butyl bromide (HBB) and three different alpha-1 blockers in the treatment of distal ureteral stones.A total of 140 patients with stones located in the distal tract of the ureter...

Synonyms

Terazosin Hydrochloride

[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-(oxolan-2-yl)methanone

MFCD00467965

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