Sarpogrelate (former developmental code names MCI-9042, LS-187,118) is a

drug A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug i ...

which acts as an

antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.serotonin Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...

5-HT_2A 5-HT_2B, and 5-HT_2C receptors. However, its affinities for the human 5-HT_2C and 5-HT_2B receptors are about one and two orders of magnitude lower than for the human 5-HT_2A receptor, respectively. The drug blocks

serotonin Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...

-induced

platelet aggregation Platelets or thrombocytes () are a part of blood whose function (along with the coagulation factors) is to react to bleeding from blood vessel injury by clumping to form a blood clot. Platelets have no cell nucleus; they are fragments of cytop ...

, and has potential applications in the treatment of many diseases including

diabetes mellitus Diabetes mellitus, commonly known as diabetes, is a group of common endocrine diseases characterized by sustained hyperglycemia, high blood sugar levels. Diabetes is due to either the pancreas not producing enough of the hormone insulin, or th ...

Buerger's disease Thromboangiitis obliterans, also known as Buerger disease (English ; ) or Winiwarter-Buerger disease, is a recurring progressive inflammation and thrombosis (clotting) of small and medium arteries and veins of the hands and feet. It is strongly ...

Raynaud's disease Raynaud syndrome, also known as Raynaud's phenomenon, is a medical condition in which the spasm of small arteries causes episodes of reduced blood flow to end arterioles. Typically the fingers, and, less commonly, the toes, are involved. Rare ...

coronary artery disease Coronary artery disease (CAD), also called coronary heart disease (CHD), or ischemic heart disease (IHD), is a type of cardiovascular disease, heart disease involving Ischemia, the reduction of blood flow to the cardiac muscle due to a build-up ...

angina pectoris 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 part ...

, and

atherosclerosis Atherosclerosis is a pattern of the disease arteriosclerosis, characterized by development of abnormalities called lesions in walls of arteries. This is a chronic inflammatory disease involving many different cell types and is driven by eleva ...

. The predicted

log P Log most often refers to: * Trunk (botany), the stem and main wooden axis of a tree, called logs when cut ** Logging, cutting down trees for logs ** Firewood, logs used for fuel ** Lumber or timber, converted from wood logs * Logarithm, in mathem ...

( XLogP3) of sarpogrelate is 1.2. A 2004 review stated that it was unknown whether sarpogrelate crosses the

blood–brain barrier The blood–brain barrier (BBB) is a highly selective semipermeable membrane, semipermeable border of endothelium, endothelial cells that regulates the transfer of solutes and chemicals between the circulatory system and the central nervous system ...

. However, other papers have stated that sarpogrelate minimally crosses into the brain and hence is peripherally selective. Accordingly, a rat study found that peak sarpogrelate levels were 50-fold lower in the brain and spinal cord than in the circulation.

References

{{Serotonin receptor modulators 3-Methoxyphenyl compounds Abandoned drugs 5-HT2A antagonists 5-HT2B antagonists 5-HT2C antagonists Carboxylate esters Dimethylamino compounds Peripherally selective drugs Phenol ethers Succinates

See also

References