Reserpine pharmacological properties

Reserpine (1) with its remarkable pharmacological properties remains an attractive synthetic target. The first total synthesis of reserpine (1), by... 

The acid-catalysed epimerization reaction often contributes to the change of conformation that alters the sterical shape of a compound. This may have a severe effect on pharmacological properties as with reserpine (1) and isoreserpine (2). The same seems to apply to the C-3 epimers yohimbine (78) and pseudoyohimbine (79). Yohimbine (78) blocks ai-receptors, whereas pseudoyohimbine (79) has little affinity for this... 

Erickson JD, Eiden LE, Hoffman BJ (1992) Expression cloning of a reserpine-sensitive vesicular monoamine transporter. Proc Natl Acad Sci USA 89 10993-10997 Erickson JD, Schafer MK, Bonner TI, Eiden LE, Weihe E (1996) Distinct pharmacological properties and distribution in neurons and endocrine cells of two isoforms of the human vesicular monoamine transporter. Proc Natl Acad Sci USA 93 5166-5171 Faham S, Watanabe A, Besserer GM, Cascio D, Specht A, Hirayama BA, Wright EM, Abramson J (2008) The crystal structure of a sodium galactose transporter reveals mechanistic insights into Na+/sugar symport. Science 321 810-814... 

The review of the history of reserpine and vincaleukoblastine reveals that each alkaloid was a minor constituent of a complex mixture and that its isolation from the mixture was guided in each case by assay for characteristic pharmacological properties. It is likely that, had the investiga-... 

Reserpine possesses one outstanding pharmacological property it releases the monoamines from both their central and peripheral storage sites. The other noteworthy property of reserpine is its parasympathomimetic action which leads to hypotension, bradycardia, miosis and hypothermia. ... 

A review article on certain aspects of the pharmacological properties of most of the iboga alkaloids has appeared (41). Several compounds stimulated the central nervous system in a way which was not amphetamine-like and manifested itself in a number of cases as antagonism against the reserpine catalepsy. Many of the compounds caused hypotension and bradycardia in anesthetized cats. Under these conditions ibogaline was the most active alkaloid. Coronaridine is said to produce a significant diuresis (42) and catharanthine has some hypoglycemic activity (43). 

The pharmacological properties of rescinnamine are similar to those of reserpine, bnt... 

The pharmacological properties of deserpidine are similar to those of reserpine, causing sedation and tranquilization. Toxic effects from high doses include drowsiness, depression, nansea, diarrhea, abdominal cramps, and hypotension. It is less toxic than reserpine. However, the poisoning effects may be greater than those of other Rauwolfia alkaloids, such as rescinnamine. An oral LD50 value in mice is 500 mg/kg. 

Some R. a. have valuable pharmacological properties. They may act centrally (e.g. see Reserpine) or peripherally (e g. see Yohimbine, Ajmaline). In addition to the pure alkaloids or their synthetic analogs, extracts of the drug Radix Rauwolfiae and combination preparations are also used. The drug has been known since early times in Indian folk medicine, and its systematic investigation began in 1930. 

There were several reports of new MAO inhibitors. The following compounds had, in addition to this action, some of the pharmacological properties of the antidepressants. Compound an analogue of pargyline, exhibited anti-reserpine and excitatory effects in mice 5. In a series of cyclic derivatives of N-aminoephedrine, 33. had anti-reserpine effects and... 

The normethyl derivative of imipramine displayed different pharmacologic and clinical properties from its fully methylated parent structure. In rats it increased spontaneous motor activity (73) and did not potentiate the action of reserpine in animals but rather antagonized it (26, 105). In both these respects, it thereby differed from imipramine. Its clinical onset of action was more rapid than with imipramine (73, 105), although efficacy did not appear to be increased. Side effects were less severe and their nature also different (58, 78). 

Stimulant effect was reported [302]. In pharmacological tests, (119) potentiated many adrenaline like compounds and antagonized reserpine, tetrabenazine and phenothiazine. It has no anticholinergic, depressive, analgesic or local anaesthetic properties [303]. Notwithstanding structural analogy with harmaline (120), data on MAO inhibition were not presented. 

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