Glyceryl 1-nitrate (G-1-N) is an intermediate metabolic product in the stepwise de-esterification of glyceryl trinitrate (GTN) in animals and humans. It belongs to the group of orally effective longacting antianginal nitrates. In anesthetized rabbits, intravenous (L) G-1-N reduced the blood pressure slightly more than (D) G-1-N, while in the conscious dog the blood pressure lowering effect of (D) G-1-N was greater and had a much longer duration (4-6 versus 2 h) than that of (L)G-1-N. The differences in dogs are probably explained by enantiospecific pharmacokinetics: (D) G-1-N had higher plasma levels and showed a longer half-life of elimination than (L) G-1-N. From the pharmacokinetic point of view, the drug offers clear advantage over glyceryl trinitrate in clinical use: G-1-N is orally available - owing to its relatively low clearance it stays much longer in the body than GTN - kinetic parameters are predictable with low coefficients of variation - and the denitration products of G-1-N are expected to be pharmacologically neutral.

Isosorbide 2-mononitrate is a pharmacologically active metabolite of isosorbide dinitrate, an organic nitrate isosorbide dinitrate indicated for the prevention of angina pectoris due to coronary artery disease. It activates guanylate cyclase.

Tropine is a naturally-occurring tropane alkaloid, which can be obtained from tropinone under the action of Tropinone reductases I. Tropine serves as an intermediate in the synthesis of different bioactive alkaloids, including atropine. In 1950th was published an article, where was described the use tropine in the treatment of angina pectoris. But in further articles were mentioned the derivative of tropine, atropine for the treatment of this disease.

Visnagin is furanochromone and one of the main compounds of Ammi visnaga L. (syn. Khella) that can be frequently found in ethnomedical formulations in Asia and the Middle East. Visnagin possess analgesic properties due to its calcium channel blocking properties and act in an anti-inflammatory manner by inhibiting AP-1 and NF-κB signaling.

Lysing is an essential basic amino-acid encoded by codone AAA and AAG, and used in the biosynthesis of proteins. The daily requirement for lysine is 38 mg/kg body weight. The most rich source of lysine is fish, beef, chicken. In a clinical study lysine supplements was found to be an effective for reduction of occurrence, severity and healing time for recurrent HSV infection, however Cochrane Review concluded that the evidence is insufficient. Lysine was investigated for improving anxiety, ameliorating angina prectoris. Lysine acetylsalicylate has been used to treat pain and to detoxify the body after heroin use. Lysine clonixinate has been used for its analgesic properties for the treatment of migraine headaches and other painful conditions. However, limited clinical trials exist for these conditions.

Dimoxyline is the synthetic analogue of papaverine, Acute toxicity studies show it to be less toxic than papaverine. No analgesic action and no tolerance development in experimental animals by repeated administration. But Dimoxyline does not appear to be as potent as papaverine in comparable dosage. Dimoxyline is indicated for the treatment of patients with angina pectoris. Also, significant amount of benefit was claimed in patients with acute or chronic phlebitis, arterial thrombosis or embolism, Raynaud’s phenomena and early thromboangiitis obliterans or arteriosclerosis obliterans. Detected adverse events are: nausea or abdominal cramps.

Khellin is a crystalline extract of a crude drug, which has long been used in Egypt for the treatment of ureteral colic. It is used in the management of bronchial asthma and angina pectoris. Interest in khellin as an adjunct to ultraviolet (UV) light therapy in the treatment of vitiligo is based on the structural similarity between khellin and the psoralens. Success has been reported using oral and topical khellin in clinical studies but it is not likely that khellin will be approved for the treatment of vitiligo. Unwanted side effects of khellin include dizziness, reversible cholestatic jaundice, pseudoallergic reaction, and elevated levels of liver enzymes (transaminases and gamma-glutamyltransferase).

Theobromine is the primary alkaloid present in the cocoa and chocolate. Theobromine is found in the shells and beans of the cacao plant and it is extracted from the husks of the bean and used for the synthesis of caffeine. Theobromine is an adenosine A1 and A2a receptor antagonist. Thesodate is used as a vasodilator, a diuretic, and heart stimulant. And similar to caffeine, it may be useful in management of fatigue and orthostatic hypotension. The symptomatic adverse reactions produced by theobromine are more or less tolerable and if they become severe, they can be treated symptomatically, these include anxiety, restlessness, tremors, sleeplessness, nausea and vomiting, loss of appetite. Theobromine is currently not in use as a medicinal drug.

Amoproxan (Mederel, Mexderel), a coronary artery dilator and anti-arrhythmic, apparently withdrawn from production, produced pellagroid skin changes and several cases of axial optic neuropathy in France.

Bepridil (trade name Vascor) is an amine calcium channel blocker used to treat angina. Bepridil is a calcium channel blocker that has well characterized anti-anginal properties and known but poorly characterized type 1 anti-arrhythmic and anti-hypertensive properties. It is not related chemically to other calcium channel blockers such as diltiazem hydrochloride, nifedipine and verapamil hydrochloride. Bepridil has inhibitory effects on both the slow calcium (L-type) and fast sodium inward currents in myocardial and vascular smooth muscle, interferes with calcium binding to calmodulin, and blocks both voltage and receptor operated calcium channels. Bepridil inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle. This has been demonstrated in isolated myocardial and vascular smooth muscle preparations in which both the slope of the calcium dose response curve and the maximum calcium-induced inotropic response were significantly reduced by bepridil. In cardiac myocytes in vitro, bepridil was shown to be tightly bound to actin. Bepridil regularly reduces heart rate and arterial pressure at rest and at a given level of exercise by dilating peripheral arterioles and reducing total peripheral resistance (afterload) against which the heart works. Bepridil is no longer sold in the United States, but it is still marketed in other countries. Bepridil has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist. Although, it contains one chiral center, it is generally administered as a racemates. The drug bepridil is a racemic mixture of two enantiomers for the 2R as CID 16048570 and 2S as CID 445143. (R)-isomer of bepridil is more active than (-S)- isomer, in certain cases. In the retrogradely perfused, paced rat heart the higher activity was found for the (+)-enantiomer, which was 4.27 times more potent in increasing coronary flow than the (-)-isomer. The two enantiomers of bepridil showed a lower activity on maximum systolic left ventricular pressure (MSLVP) than on coronary flow, and a similar 3-4 fold stereoselectivity with both parameters.