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Denopamine
Denopamine ( INN) is a cardiotonic drug which acts as a β1 adrenergic receptor agonist. It is used in the treatment of angina and may also have potential uses in the treatment of congestive heart failure Heart failure (HF), also known as congestive heart failure (CHF), is a syndrome, a group of signs and symptoms caused by an impairment of the heart's blood pumping function. Symptoms typically include shortness of breath, excessive fatigue, ... and for clearing pulmonary oedema. It is marketed in Japan under the brand name Kalgut (カルグート) and available as tablets of 5 and 10 mg, and 5% fine granules. Synthesis According to the patent, Denopamine can be used as either an antidiabetic or a cardiotonic. The reaction between 1-(4-benzyloxyphenyl)-2-chloroethanone 3365-56-0(1) and 3,4-Dimethoxyphenethylamine 20-20-7( DMPEA) (2) giveCID:10993165(3). The reduction of the ketone with sodium borohydride gavCID:12940814(4). Catalytic hydrogenation cleaves the be ...
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Denopamine Synthesis
Denopamine ( INN) is a cardiotonic drug which acts as a β1 adrenergic receptor agonist. It is used in the treatment of angina and may also have potential uses in the treatment of congestive heart failure Heart failure (HF), also known as congestive heart failure (CHF), is a syndrome, a group of signs and symptoms caused by an impairment of the heart's blood pumping function. Symptoms typically include shortness of breath, excessive fatigue, ... and for clearing pulmonary oedema. It is marketed in Japan under the brand name Kalgut (カルグート) and available as tablets of 5 and 10 mg, and 5% fine granules. Synthesis According to the patent, Denopamine can be used as either an antidiabetic or a cardiotonic. The reaction between 1-(4-benzyloxyphenyl)-2-chloroethanone 3365-56-0(1) and 3,4-Dimethoxyphenethylamine 20-20-7( DMPEA) (2) giveCID:10993165(3). The reduction of the ketone with sodium borohydride gavCID:12940814(4). Catalytic hydrogenation cleaves the be ...
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Beta-1 Adrenergic Receptor
The beta-1 adrenergic receptor (β1 adrenoceptor), also known as ADRB1, is a beta-adrenergic receptor, and also denotes the human gene encoding it. It is a G-protein coupled receptor associated with the Gs heterotrimeric G-protein and is expressed predominantly in cardiac tissue. Receptor Actions Actions of the β1 receptor include: The receptor is also present in the cerebral cortex. Agonists Isoprenaline has higher affinity for β1 than adrenaline, which, in turn, binds with higher affinity than noradrenaline at physiologic concentrations. Selective agonists to the beta-1 receptor are: *Denopamine * Dobutamine (in cardiogenic shock) *Xamoterol (cardiac stimulant) Antagonists ''(Beta blockers)'' β1-selective antagonists include: *Acebutolol (in hypertension, angina pectoris and arrhythmias) *Atenolol (in hypertension, coronary heart disease, arrhythmias and myocardial infarction) *Betaxolol (in hypertension and glaucoma) *Bisoprolol (in hypertension, coronary h ...
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Japan
Japan ( ja, 日本, or , and formally , ''Nihonkoku'') is an island country in East Asia. It is situated in the northwest Pacific Ocean, and is bordered on the west by the Sea of Japan, while extending from the Sea of Okhotsk in the north toward the East China Sea, Philippine Sea, and Taiwan in the south. Japan is a part of the Ring of Fire, and spans an archipelago of 6852 islands covering ; the five main islands are Hokkaido, Honshu (the "mainland"), Shikoku, Kyushu, and Okinawa. Tokyo is the nation's capital and largest city, followed by Yokohama, Osaka, Nagoya, Sapporo, Fukuoka, Kobe, and Kyoto. Japan is the eleventh most populous country in the world, as well as one of the most densely populated and urbanized. About three-fourths of the country's terrain is mountainous, concentrating its population of 123.2 million on narrow coastal plains. Japan is divided into 47 administrative prefectures and eight traditional regions. The Greater Tokyo ...
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Tablet (pharmacy)
A tablet (also known as a pill) is a pharmaceutical oral dosage form (''oral solid dosage'', or OSD) or solid unit dosage form. Tablets may be defined as the solid unit dosage form of medicament or medicaments with suitable excipients. It comprises a mixture of active substances and excipients, usually in powder form, pressed or compacted from a powder into a solid dose. Tablets are prepared either by molding or by compression. The excipients can include diluents, binders or granulating agents, glidants (flow aids) and lubricants to ensure efficient tabletting; disintegrants to promote tablet break-up in the digestive tract; sweeteners or flavours to enhance taste; and pigments to make the tablets visually attractive or aid in visual identification of an unknown tablet. A polymer coating is often applied to make the tablet smoother and easier to swallow, to control the release rate of the active ingredient, to make it more resistant to the environment (extending its shel ...
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Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive


Types of agonists

can be activated by either endogenous agonists (such as
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Angina
Angina, also known as angina pectoris, is chest pain or pressure, usually caused by insufficient blood flow to the heart muscle (myocardium). It is most commonly a symptom of coronary artery disease. Angina is typically the result of obstruction or spasm of the arteries that supply blood to the heart muscle. The main mechanism of coronary artery obstruction is atherosclerosis as part of coronary artery disease. Other causes of angina include abnormal heart rhythms, heart failure and, less commonly, anemia. The term derives from the Latin ''angere'' ("to strangle") and ''pectus'' ("chest"), and can therefore be translated as "a strangling feeling in the chest". There is a weak relationship between severity of angina and degree of oxygen deprivation in the heart muscle, however, the severity of angina does not always match the degree of oxygen deprivation to the heart or the risk of a myocardial infarction (heart attack). Some people may experience severe pain even thou ...
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Heart Failure
Heart failure (HF), also known as congestive heart failure (CHF), is a syndrome, a group of signs and symptoms caused by an impairment of the heart's blood pumping function. Symptoms typically include shortness of breath, excessive fatigue, and leg swelling. The shortness of breath may occur with exertion or while lying down, and may wake people up during the night. Chest pain, including angina, is not usually caused by heart failure, but may occur if the heart failure was caused by a heart attack. The severity of the heart failure is measured by the severity of symptoms during exercise. Other conditions that may have symptoms similar to heart failure include obesity, kidney failure, liver disease, anemia, and thyroid disease. Common causes of heart failure include coronary artery disease, heart attack, high blood pressure, atrial fibrillation, valvular heart disease, excessive alcohol consumption, infection, and cardiomyopathy. These cause heart failure by alterin ...
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Pulmonary Oedema
Pulmonary edema, also known as pulmonary congestion, is excessive liquid accumulation in the tissue and air spaces (usually alveoli) of the lungs. It leads to impaired gas exchange and may cause hypoxemia and respiratory failure. It is due to either failure of the left ventricle of the heart to remove oxygenated blood adequately from the pulmonary circulation (cardiogenic pulmonary edema), or an injury to the lung tissue directly or blood vessels of the lung (non-cardiogenic pulmonary edema). Treatment is focused on three aspects: firstly improving respiratory function, secondly, treating the underlying cause, and thirdly preventing further damage and assuring full recovery to the lung. Pulmonary edema, especially when sudden (acute), can lead to respiratory failure or cardiac arrest due to hypoxia. It is a cardinal feature of congestive heart failure. The term edema is from the Greek (''oidēma'', "swelling"), from οἰδέω (''oidéō'', "(I) swell"). Types Classically ...
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DMPEA
DMPEA can refer to two subclasses of substituted phenethylamines: Dimethoxy-phenethylamines * 2,3-Dimethoxyphenethylamine * 2,4-Dimethoxyphenethylamine * 2,5-Dimethoxyphenethylamine * 2,6-Dimethoxyphenethylamine * 3,4-Dimethoxyphenethylamine 3,4- Di methoxy phenethylamine (DMPEA) is a chemical compound of the phenethylamine class. It is an analogue of the major human neurotransmitter dopamine where the 3- and 4-position hydroxy groups have been replaced with methoxy groups. It is ... (homoveratrylamine) * 3,5-Dimethoxyphenethylamine Dimethyl-phenethylamines * α,α-Dimethylphenethylamine (Phentermine) * ''N'',α-Dimethylphenethylamine (Methamphetamine) * 2,α-Dimethylphenethylamine (Ortetamine) * 3,α-Dimethylphenethylamine * 4,α-Dimethylphenethylamine * ''N'',''N''-Dimethylphenethylamine {{Chemistry index ...
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