Etilefrine is a cardiac stimulant used as an antihypotensive. Intravenous infusion of this compound increases cardiac output, stroke volume, venous return and blood pressure in man and experimental animals, suggesting stimulation of both α and β adrenergic receptors. However, in vitro studies indicate that etilefrine has a much higher affinity for β1 (cardiac) than for β2 adrenoreceptors. Intravenous etilefrine increases the pulse rate, cardiac output, stroke volume, central venous pressure and mean arterial pressure of healthy individuals. Marked falls in pulse rate, cardiac output, stroke volume and peripheral bloodflow, accompanied by rises in mean arterial pressure, occur when etilefrine is infused after administration of intravenous propranolol 2,5 mg. These findings indicate that etilefrine has both β1 and α1 adrenergic effects in man. The French Health Products Agency concluded that etilefrine and heptaminol have an unfavourable harm-benefit balance, and also placed restrictions on the use of midodrine.

Denopamine is a selective agonist of beta-1 adrenergic receptor. The drug was approved in Japan under the name Kalgut for the treatment of chronic heart failure.

Lopinavir D-Valine Diastereomer, a selective HIV protease inhibitor, possesses similar properties with lopinavir.

Dimetofrine is a selective agonist of post-synaptic a1-adrenergic receptors. The drug was investigated as a cardiostimulant to treat orthostatic hypotension. Clinical investigation showed that dimetofrine relieves asthenia, paleness, drowsiness, fatigue, headache and other symptoms associated with hypotension. It was observed, that in acidic conditions similar to conditions in the stomach, dimetofrine is able to react with nitrites with the formation of highly mutagenic compound 2,6-dimethoxy-1,4-benzoquinone (DMBQ).

Butoxamine is a selective antagonist of the beta2 adrenergic receptor. It was discovered in laboratories of Farbwerke Hoechst. Administration of 25-50 mg subcutaneously or 50-150 mg orally induced mescaline syndrome, disorders of consciousness and a psychotic episode with amnesia. At an oral dose of 5 mg, butoxamine inhibited metabolic changes induced by fasting and administration of catecholamines. Butoxamine was not developed further and is mainly used in biomedical research to study the functional role of beta2 receptors.

Tribenoside, a glucofuranoside derivative has been shown to have potent anti-allergic and anti-inflammatory properties. It has been reported to display a pluripotent antagonistic action against histamine, serotonin, bradykinin and other inflammatory substances. Tribenoside decrease capillary permeability, thus reducing edema. Tribenoside combat the pathological processes of capillaries and veins. It is used in adults and adolescents for treatment of venous circulation diseases. Although Tribenoside is derived from a sugar substance, it doesn’t affect the carbohydrate metabolism even in diabetics. Tribenoside might cause some side effects such as skin redness, headache. Very rare cases are: systemic anaphylaxis, including urticaria, angioedema.

Diiodohydroxypropane was once used as an antiseptic and disinfectant. Diiodohydroxypropane was investigated in the therapy of gingival bacteroiditis.

A potent, selective and orally active receptor antagonist of leukotriene D4, verlukast (MK-571), was discovered and developed from a styrylquinoline lead structure based on a hypothetical model of the leukotriene D4 receptor. MK-571 blocks the action of LTD4 in animals and man, and is effective in a number of animal models of antigen-induced bronchoconstriction at plasma concentration at or below 2 ug/mL. MK-571 also blocks antigen-induced asthmatic responses in man. MK-571 is a potent and selective leukotriene D4 (LTD4) antagonist and ABCC multidrug resistance protein 1(MRP1) inhibitor. The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, mediate their actions through two distinct G-protein coupled receptors. LTD4 is the preferred ligand for the CysLT1 receptor, whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor. MK-571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively. MK-571 effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors.

Benidipine is an orally triple L-, T-, and N-type calcium channel blocker for the treatment of hypertension and angina pectoris synthesized and developed by Kyowa Hakko Kogyo Co., Ltd. Benidipine, approved in Japan in November 1991, has become one of the three best selling CCBs and is highly useful as a potent, long-lasting antihypertensive and antianginal agent.

Mabuterol is a long acting βeta 2-adrenergic agonist which stimulates adenylyl cyclase activity and the closing of calcium channels. Studies indicate that the R enantiomer of mabuterol is more potent than the S enantiomer. In addition, the half-life is longer in the R enantiomer than the S. Studies conducted on rats and dogs show that mabuterol acts as a bronchodilator. At high concentrations mabuterol can also antagonize beta1 adrenoceptors in guinea pigs