Coronary dilation,

The possible therapeutic applications of these alkaloids as proto-zooicidal agents, coronary dilators and ecbolics, and in nervous diseases, for example in the treatment of post-encephalitic conditions, have been discussed by a number of authors. The alkylharmols, referred to above, form part of an extensive series prepared by Coulthard, Levene and Pyman, and tested by these authors for bactericidal properties and by... 

Early reports of analgesic and antiarthritic activity in octahydropjTido[4,3-d]pyrimidines do not appear to have been substantiated, but a number of recent patents refer to the antipyretic, diuretic, bacteriostatic, sedative, and coronary-dilating activities of a series of 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidines. Pharmacological properties claimed for, 5,6-dihydropyrido[2,3-[Pg.198]

Drugs with a-adrenergic blocking activity are peripheral coronary-dilating agents that only differ in specificity with aj-adrenergic receptors. Prazozin and tetrazin are selective aj-adrenoblockers that are used in therapeutic doses to lower arterial pressure. 

Pharmacology The principal pharmacological action of nitrates is relaxation of the vascular smooth muscle and consequent dilation of peripheral arteries and especially the veins. Dilation of the veins promotes peripheral pooling of blood and decreases venous return to the heart, thereby reducing left ventricular end-diastolic pressure and pulmonary capillary wedge pressure (preload). Arteriolar relaxation reduces systemic vascular resistance, systolic arterial pressure, and mean arterial pressure (afterload). Dilation of the coronary arteries also occurs. The relative importance of preload reduction, afterload reduction, and coronary dilation remains undefined. 

It is a coronary dilator and claimed to dilate coronary resistance vessels. It probably... 

Nitroglycerine 10a is both a drug and an explosive. Its inclusion into the cavity of p-cyclodextrin, p-CD, 11 prevents its decomposition and enhances its bioavailability [14]. The complex of 10a with 11 is marketed under the name Nitropen as a coronary dilator sublingual tablets by Nippon Kayaku company in Japan. 

Oxidizing degradation (H202) of the same furochromones leads to the corresponding benzofuran-5-carboxylic acids.857,858 Similarly, alkaline degradation of 418, a dehydration product of visamminol (417) (a natural coronary dilator) leads to benzofuran (419) and acetone.859... 

Many substituted benzofurans show marked pharmacological activity. 2-(4-Hydroxyben-zoyl)benzofuran exhibits a relaxant effect on histamine and acetylcholine spasm. 2-Ethyl-3 -(4-hydroxy-3,5-diiodobenzyl)benzofuran has been shown to be superior to khellin as a coronary dilator. 2-Butyl-3-benzoylfuranyl 4-diethylaminoethoxy-3,5-diiodophenyl ketone, an anginal drug which causes coronary dilation, depresses myocardial oxygen consumption (74HC(29)l). 

The enzyme in the myocardium has recently attracted attention because of the possibility that adenosine is a physiological regulator of coronary blood flow (67) (adenosine is a potent coronary dilator). Most of the 5 -nucleotidase activity in rat heart is membrane bound, and a partially purified preparation has been obtained by extracting acetone powder preparations with deoxycholate (68). All 5 -nucleotides are hydrolyzed. The enzyme is strongly inhibited competitively by ATP (Ki 1.8 fxM). Whether this provides a regulatory mechanism for adenosine formation in the heart is not known. 

A series of esters of nuclear halogenated 3-carboxy-1,2,3-benzotriazin-4(3//)-ones show depressant activity, while the benzoate esters of substituted 3-(2-hydroxyethyl)-l,2,3-benzotriazin-4(3fl)-one are reported to function as coronary dilating agents,262 as do certain other compounds of this type.263 3-(o-Haloaryl)-1,2,3-benzotriazin-4(3//)-ones are claimed to have antisecretory,264 anoretic, anticonvulsant, and hypoglycemic265 activity, and a variety of other 3-aryl derivatives are stated to be relaxants, tranquilizers, sedatives, hypnotics, or cramp inhibitors.266 A number of derivatives of 10, R = H, in which the 3-substituent is a long alkyl chain containing a terminal sulfonamide group have been claimed to act. as antidiabetics.267... 

Hanna and Shutt (146) studied the relationship between the chemical structure and the coronary dilator action of papaverine analogs on anesthetized dogs. The 6-alkoxy-, 5,6-dialkoxy-, and 6,7-dialkoxy-isoquinoline derivatives acted as dilators. The 6,7-dialkoxyisoquinoline derivatives were most effective. Optimum results were obtained when the isoquinoline nucleus was aromatic, but the 3,4-dihydro- and 1,2,3,4-... 

Angiotensin-converting enzyme inhibitors have been tested for possible prevention of the restenosis that frequently occurs after coronary dilation. These studies were undertaken based on an experimental... 

Amiodarone, for example (Fig. 1.12), was introduced as a coronary dilator for angina, but concern about comeal deposits, discoloration of skin exposed to sunlight and thyroid disorders led to the withdrawal of the drug in 1967. However, in 1974 amiodarone was found to be highly effective in the treatment of a rare type of arrhythmia known as the Wolff-Parkinson-White syndrome. Accordingly, amiodarone was reintroduced specifically for that purpose [22]. 

Benziodarone was initially used in Europe as a coronary dilator, and proved later to be a useful uricosuric agent However, it is now withdrawn from the market due to several cases of jaundice associated with its use [22]. The corresponding brominated analogue, benzbromarone was specifically marketed for its uricosuric properties. 

Exertional angina calcium antagonists are useful in the treatment of exercise-induced angina, through their ability to increase coronary dilatation and blood flow. 

The title theophylline isotopomers 28 and 29, 2,6-dihydro- 1,3-dimethylpurines, are alkaloids known for their diuretic, cardiotonic and coronary-dilating properties, and are used at present in therapeutics as a bronchodilators in all kinds of asthma12. They have... 

A number of compounds have been reported which have coronary dilator properties or other activities which have culminated in their clinical trial for use in angina pectoris. Lidoflazlne (IV) is claimed to be a specific, long acting coronary vasodilator. This agent appears to reduce coronary vascular resistance in dogs and causes an Increase in coronary venous pO. ... 

Theobromine is extracted from the shells of cocoa-seeds. Theobromine has no centrally stimulant action but instead it is a diuretic and it has coronary dilating effects, effects. 

---