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Ketanserin

Ketanserin structure

CAS No:
74050-98-9
Formula:
C22H22FN3O3
Chemical Name:
Ketanserin
Synonyms:
2,4(1H,3H)-Quinazolinedione,3-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-;3-[2-[4-(4-Fluorobenzoyl)-1-piperidinyl]ethyl]-2,4(1H,3H)-quinazolinedione;R 41468;Ketanserin;Ketensin;Vulketan Gel;Suffrexal;78168-89-5
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

Ketanserin is a selective 5-HT receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).

Ketanserin is a member of the class of quinazolines that is quinazoline-2,4(1H,3H)-dione which is substituted at position 3 by a 2-[4-(p-fluorobenzoyl)piperidin-1-yl]ethyl group. It has a role as an alpha-adrenergic antagonist, a serotonergic antagonist, an antihypertensive agent, a cardiovascular drug and an EC 3.4.21.26 (prolyl oligopeptidase) inhibitor. It is a member of quinazolines, a member of piperidines, an organofluorine compound and an aromatic ketone.|Ketanserin has been investigated for the treatment of Septic Shock, Severe Sepsis, and Diabetic Foot Ulcer.|Ketanserin is a quinazoline derivative and serotonin (5-hydroxytryptamine, 5HT) receptor subtype 2 (5-HTR2) antagonist with potential antihypertensive and antiplatelet activities. Following administration, ketanserin binds to and inhibits the signaling mediated by 5-HTR2, which inhibits serotonin-dependent vasoconstriction and platelet activation.|A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.

Ketanserin Basic Attributes

Molecular Weight：

395.43

Exact Mass：

395.43

EC Number：

277-680-2

UNII：

97F9DE4CT4

NSC Number：

758959

DSSTox ID：

DTXSID3023188

NCI Thesaurus Code：

C604

ATC Code：

C - Cardiovascular system

HScode：

2933990090

Characteristics

PSA：

69.7

XLogP3：

2.6

Density：

1.3±0.1 g/cm3

Melting Point：

231 °C

Refractive Index：

1.593

Water Solubility：

DMF: 10 mg/mL, clear, colorless

Storage Conditions：

2-8°C

Safety Information

wgk germany：

RTECS Number：

VA1411190

Precautionary statement(s)：

P264, P270, P301+P312, P330, P501

Hazard Statements：

H302

GHS Classification：

|Danger|H301 (82.98%): Toxic if swallowed [Danger Acute toxicity, oral]|P264, P270, P301+P310, P301+P312, P321, P330, P405, and P501|Aggregated GHS information provided by 47 companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P264, P270, P301+P312, P330, and P501|Aggregated GHS information provided by 97 companies from 1 notifications to the ECHA C&L Inventory.

Drug Information

MeSH：

Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS. (See all compounds classified as Serotonin Antagonists.)|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. (See all compounds classified as Antihypertensive Agents.)|Drugs or agents which antagonize or impair any mechanism leading to blood platelet aggregation, whether during the phases of activation and shape change or following the dense-granule release reaction and stimulation of the prostaglandin-thromboxane system. (See all compounds classified as Platelet Aggregation Inhibitors.)

MeSH Entry Terms：

3-(2-(4-(4-Fluorobenzoyl)piperidinol)ethyl)-2,4(1H,3H)-quinazolinedione

Ketanserin Use and Manufacturing

An antihypertensive, with affinity for multiple GPCR receptors.

Computed Properties

Molecular Weight:395.4
XLogP3:2.6
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:5
Exact Mass:395.16451973
Monoisotopic Mass:395.16451973
Topological Polar Surface Area:69.7
Heavy Atom Count:29
Complexity:627
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Material

2-Pentanone

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