Meptazinol is a unique opioid analgesic. Binding studies suggest a relative selectivity for mu-1 opioid receptor sites. Meptid is indicated for the treatment of moderate to severe pain, including post-operative pain, obstetric pain and the pain of renal colic. The most commonly reported adverse reactions after treatment with meptazinol are nausea, vomiting, dizziness, diarrhoea and increased sweating, constipation, abdominal pain, rash, vertigo, headache, drowsiness, somnolence and dyspepsia.

Bambuterol is an active precursor of the selective beta2-adrenergic agonist terbutaline. Bambuterol is the bis-N,N-dimethyl-carbamate of terbutaline. Bambuterol is a remarkably selective and potent inhibitor of cholinesterase. BAMBEC (Bambuterol hydrochloride) oral solution or tablets are indicated for the management of asthma, bronchospasm and/or reversible airways obstruction.

Romurtide (Muroctasin) is a non-specific immune stimulant derived from muramyl dipeptide, which is obtained from gram-positive bacterial cell walls. Muroctasin stimulates macrophages, which release interleukin-l, which in turn increases production of colony-stimulating factors; muroctasin also evokes an increased production of neutrophils. It is used in Japan for chemotherapy-induced leukopenia.

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.

Penequinine (penehyclidine) is a selective M1/M2 receptor antagonist. Due to anticholinergic effects, penequinine is used in Chine for the treatment of organophosphorus and soman poisoning. In addition, penequinine is a negative regulator of TLR4 and NF-kB signaling and is investigated as a potential treatment in clinical trials for the treatment of acute lung injury and acute cerebral ischemia-reperfusion injury.

(R)-Lercanidipine is enantiomer of antihypertensive drugs Lercanidipine, that acts by blocking L-type calcium channels, allowing relaxation and opening of blood vessels. The dihydropyridine calcium antagonists promote systemic vasodilatation by a reversible blockade of voltagedependent Ca2+ influx through L-type channels in the cell membrane. (S)-Lercanidipine has 100- to 200-fold greater affinity than the (R)-enantiomer for the L-type calcium channel. The pharmacokinectics of (S)- Lercanidipine has been evaluated in healthy volunteers, in elderly and non-elderly patients with hypertension, and in patients with renal or hepatic impairment. Patients from these studies were investigated after receiving a single 10 or 20 mgdose of [14C]-labeled rac-Lercanidipine as a solution. The maximum plasma concentrations of (S)-Lercanidipine were reached within 2–3 h and the area under the plasma concentration–time curves were not linearly related to the dose, indicating a saturable first-pass metabolism. The absorption of (S)-LER increases after the ingestion of a highfat meal. Lercanidipine is highly bound to plasma protein (>98%) in humans. Its volume of distribution of 2–2.5 L/kg was determined in healthy volunteers after intravenous infusion of 2 mg. Lercanidipine is extensively metabolized by CYP 3A4 to inactive pyridine derivatives. A crossover study involving a single administration of either 10 mg of (R)- or (S)-LER or 20 mg of rac-LER as a solution demonstrated no in vivo enantiomer interconversion

(S)-Lercanidipine is enantiomer of antihypertensive drugs Lercanidipine, that acts by blocking L-type calcium channels, allowing relaxation and opening of blood vessels. The dihydropyridine calcium antagonists promote systemic vasodilatation by a reversible blockade of voltage-dependent Ca2+ influx through L-type channels in the cell membrane. (S)-Lercanidipine has 100- to 200-fold greater affinity than the (R)-enantiomer for the L-type calcium channel. The pharmacokinetics of (S)- Lercanidipine has been evaluated in healthy volunteers, in elderly and non-elderly patients with hypertension, and in patients with renal or hepatic impairment. Patients from these studies were investigated after receiving a single 10 or 20 mg dose of [14C]-labeled rac-Lercanidipine as a solution. The maximum plasma concentrations of (S)-Lercanidipine were reached within 2–3 h and the area under the plasma concentration-time curves were not linearly related to the dose, indicating a saturable first-pass metabolism. The absorption of (S)-LER increases after the ingestion of a high-fat meal. Lercanidipine is highly bound to plasma protein (>98%) in humans. Its volume of distribution of 2–2.5 L/kg was determined in healthy volunteers after intravenous infusion of 2 mg. Lercanidipine is extensively metabolized by CYP 3A4 to inactive pyridine derivatives. A crossover study involving a single administration of either 10 mg of (R)- or (S)-LER or 20 mg of rac-LER as a solution demonstrated no in vivo enantiomer interconversion

levomethadone, or R-(−)-methadone, is the active enantiomer of methadone; having approximately 50x the potency of the S-(+)-enantiomer as well as greater μ-opioid receptor selectivity.

Higenamine HCl (norcoclaurine) is a plant-based alkaloid widely used as nutritional supplement in food and beverage industries. It exists in variety of plants including Tinospora crispa, Nandina domestica, Gnetum Parvifolium C.Y. Cheng, sarum Heterotropoides, Nelumbo nucifera. It was initially isolated from Aconitum and identified as the active cardiotonic component of this medicinal plant used as local and traditional medicines in many Asian regions for the treatment of various diseases such as collapse, syncope, painful joints, oedema, bronchial asthma etc. Various pharmacological properties and potentially multi-spectral medical applications of higenamine have been reviled in many in vitro and in vivo studies conducted in animals and humans. Pharmacological properties of higenamine include positive inotropic and chronotropic effect, activating slow channel effect, vascular and tracheal relaxation effect, anti-thrombotic, anti-apoptotic and anti-oxidative effect, anti-inflammatory and immunomodulatory effect. Studies on higenamine showed potential therapeutic effects for diseases like heart failure, disseminated intravascular coagulation (DIC), shock, arthritis, asthma, ischemia/reperfusion injuries and erectile dysfunction. Higenamine has been tested as a candidate of pharmacologic stress agent in the detection of coronary artery diseases (CADs) in human clinical studies in China. In animal models, higenamine has been demonstrated to be a β2 adrenoreceptor agonist. It partly exerts its actions by the activation of adenylate cyclase, responsible for boosting the cellular concentrations of the adrenergic second messenger, cAMP. Via a beta-adrenoceptor mechanism higenamine, induced relaxation in rat corpus cavernosum, leading to improved vasodilation and erectile function. Related to improved vasodilatory signals, higenamine has been shown to possess antiplatelet and antithrombotic activity via a cAMP-dependent pathway, suggesting it may contribute to enhanced vasodilation and arterial integrity. Anti-apoptotic and cardiac protective effects of higenamine were shown to be mediated by the β2-AR/PI3K/AKT cascade. Higenamine is marketed as a dietary supplement for weight loss and sport performance, and is added to many fat burning supplements. Along with many other β2 agonists, higenamine is prohibited by World Anti-Doping Agency for use in sports.