Histapyrrodine was investigated as a neuro-sedative drug for the treatment of anxiety and states of aggression.

Clorprenaline is a β2-adrenergic receptor agonist. As a bronchodilator it has been used for the treatment of bronchial asthma, bronchitis and other respiratory diseases. It is a potential new lean meat-boosting feed additive because it can promote animal muscular mass growth and decrease fat accumulation.

Bopindolol (4-[benzoyloxy-3-tertbutylaminopropoxy]-2-methylindole hydrogen malonate) is an indole beta-adrenoceptor antagonist bearing a benzoyl ester residue on the beta-carbon atom of the propanolamine side chain. Bopindolol is metabolized by esterase to benzoic acid and an active metabolite, 18-502 [4-(3-t-butylamino-2-hydroxypropoxy)-2-methyl indole], which is further metabolized to 20-785 [4-(3-t-butylaminopropoxy)-2-carboxyl indole]. Bopindolol produces sustained blockade of beta 1- and beta 2-adrenoceptors, has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is used in the treatment of hypertension. In limited trials bopindolol has also successfully reduced symptoms in patients with angina pectoris, anxiety and essential tremor.

Mitiglinide is a drug for the treatment of type 2 diabetes currently marked under tradename Glufast. Glufast® is available as the tablet for oral use, containing 5 mg or 10 mg of Mitiglinide calcium hydrate. The recommended dose is 10 mg three times daily just before each meal (within 5 minutes). Mitiglinide was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on January 29, 2004, and is currently co-marketed in Japan by Kissei and Takeda. Mitiglinide is a rapid-acting insulin secretion-stimulating agent, its belongs to the meglitinide (glinide) class of blood glucose-lowering drugs. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) (K(ATP)) channels in pancreatic beta-cells.

Meprylcaine (also known as Epirocaine and Oracaine) is a local anesthetic with stimulant properties that is structurally related to dimethocaine. Meprylcaine has a relatively potent inhibitory action on the monoamine transporter and inhibits the reuptake of dopamine, norepinephrine and serotonin. Oracaine is commonly used as the hydrochloride salt and is compatible with the known vasoconstrictors. It has a slightly more rapid onset than procaine with a slight increase in potency. The earliest symptoms of a toxic overdose are stimulation to the central nervous system, thus following the same symptoms as procaine. Not more than 400 mg. (20 ml. of a 2 per cent solution) should be used at any one time for the ambulatory patient. Oracaine, like metycaine, may be used for patients sensitive to the para-aminobenzoic acid derivatives. Oracaine hydrochloride is used at present mainly by the dental profession and in dermatologic surgery.

BENZPYRINIUM is a cholinergic drug used for prevention of postoperative intestinal atony, postoperative abdominal distention and urinary retention, or for treatment of postoperative distention.

Ractopamine hydrochloride, a beta-adrenoceptor agonist, is a phenethanolamine salt approved for use as a feed additive. Recently published studies indicate that the RR-isomer (butopamine) is the stereoisomer with the most activity at the beta-adrenoceptor. Butopamine was shown to be a non-selective ligand at the beta1 and beta2-adrenoceptors, but signal transduction is more efficiently coupled through the b2-adrenoceptor than the beta1 adrenoceptor. Therefore, the RR-isomer of ractopamine is considered to be a full agonist at the beta2-adrenoceptor and a partial agonist at the beta1¬adrenoceptor. These results are consistent with the pharmacological characterization of racemic ractopamine in isolated cardiac (atria) and smooth muscle (costo-uterine, vas deferens, trachea), which shows a maximal response at beta2- and a submaximal response at beta1¬adrenoceptors when compared with the full beta1 and beta2-adrenoceptor agonist isoproterenol. Butopamine is chemically similar to dobutamine but, unlike dobutamine, it is not a catecholamine. Butopamine induces a positive inotropic response in patients with congestive heart failure but for equal increments in cardiac output, butopamine increases heart rate more than dobutamine. Butopamine inproved cardiac performance in patients with ventricular dysfunction and congestive heart failure. Butopamine was prepared by Tuttle et al (unpublished data) and has a structure similar to dobutamine. This compound is refractory to the action of catechol-O-methyl transferase and thus it is orally active and has a longlasting action. Clinical findings in acute heart failure cases have been reported by Thompson et al. Intravenous administration produced an increase in the cardiac index and heart rate and shortening of systolic time intervals. A few patients experienced ventricular ectopy, especially with the higher doses used. No data pertaining to oral administration are available.

Clebopride is a dopamine antagonist drug. It is used to treat functional gastrointestinal disorder such as nausea or vomiting. Unchanged parent drug was the most abundant compound in human urine. Major metabolites included the hydroxylation at benzyl group to yield carbinolamine and its further N-dealkylation product, and the piperidine ring hydroxylation/oxidation metabolite (a lactam).

Acedoben (4-acetamidobenzoic acid) is a benzoic acid derivative and a metabolite of benzocaine. It is a component of immunomodulatory drug inosine pranobex, which is used to treat mucocutaneous infections due to herpes simplex virus (type 1 and/or type II), genital warts as adjunctive therapy to podophyllin or carbon dioxide laser, and subacute sclerosing panencephalitis.

Bifemelane is a psychotropic drug, was found to inhibit monoamine oxidase (MAO). It inhibited type A MAO (MAO-A) competitively and type B (MAO-B) noncompetitively and it was a more potent inhibitor of MAO-A than of MAO-B. Bifemelane is an antidepressant and cerebral activator that is used in Japan for the treatment of cerebral infarction patients with depressive symptoms, and in the treatment of senile dementia as well. It also appears to be useful in the treatment of glaucoma.