Pharmacological and Biochemical Effects of Some Reserpine Derivatives

Garattini, Silvio; Lamesta, L.; Mortari, A; Valzelli, L.

doi:10.1111/j.2042-7158.1961.tb11868.x

Cited by 18 publications

(6 citation statements)

References 2 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This suggests that reserpine inhibits ovulation because it produces changes in the CNS which are not produced by methoserpidine (Garattini, Lamesta, Mortari & Valzelli, 1961;Leroy & De Schaepdryver, 1961). A site of action for reserpine outside the CNS cannot, however, be excluded com¬ pletely because its peripheral effects are not identical with those of methoserpidine.…”

Section: Discussionmentioning

confidence: 95%

The Effect of Reserpine, 5-Hydroxytryptamine and Other Drugs on Induced Ovulation in Immature Mice

Brown¹

1966

Journal of Endocrinology

View full text Add to dashboard Cite

Ovulation was induced in immature mice by pregnant mare serum gonadotrophin. Reserpine in doses of 6\p=n-\9 \g=m\g.prevented ovulation in these animals. Methoserpidine (up to 333 \g=m\g.) did not reduce the incidence of ovulation. A single dose of 2 mg. \g=a\-methyldopa was without effect but several doses at intervals inhibited ovulation.Groups of mice treated with gonadotrophin and reserpine were pretreated with other drugs. \g=a\-Methyldopa decreased the sedative effect of reserpine but not its inhibitory effect on ovulation. Dopa antagonized both effects of reserpine.5-Hydroxytryptamine creatinine sulphate in doses of 100 or 200 \ g=m\ g. injected s.c. 16 or 17 hr. before the mice were killed consistently increased the percentage ovulating in response to gonadotrophin. A significant increase was also obtained when 5-hydroxytryptophan was injected into mice pretreated with iproniazid.

show abstract

Section: Discussionmentioning

confidence: 95%

The Effect of Reserpine, 5-Hydroxytryptamine and Other Drugs on Induced Ovulation in Immature Mice

Brown¹

1966

Journal of Endocrinology

View full text Add to dashboard Cite

show abstract

“…DL-152 has been shown to be a potent inhibitor of cyclic AMP phosphodiesterase (Honda and Imamura 1968) and to induce elevation of cyclic AMP levels in several tissues (Lehnert 1979 a, Honda andImamura 1968) . In the present study both tumours showed the same pattern of cyclic AMP changes following DL-152 administration, maximum levels being seen at 30 min after injection .…”

Section: Discussionmentioning

confidence: 98%

“…However, there are several indications that the use of this drug as an adjunct to radiotherapy is worth investigating . DL-152 is a drug which has already been used clinically and data are available as to its pharmacology in mice (Garattini et al 1961) . DL-152 is particularly effective in protecting the skin against radiation damage, and for both skin and intestine the DMF increases as dose decreases, suggesting that it would be effective in protecting against the effects of a series of small dose fractions .…”

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Radioprotection of Normal and Malignant Tissue in the Mouse by Diethylaminoreserpine

Lehnert

Fisher

Methot

1981

International Journal of Radiation Biology and Related Studies

View full text Add to dashboard Cite

The protective effect of pre-irradiation injections of diethylaminoreserpine (DL-152) for normal and malignant tissues in the mouse has been investigated. Dose modifying factors (DMFs) obtained for normal tissue ranged from 1.0 for bone marrow CFUs to more than 1.8 for skin. The DMFs for two transplantable tumours investigated were 1.0 for the EMT6 adenocarcinoma and 1.70 for the KHT fibrosarcoma (at a surviving fraction of 0.1. Acutely hypoxic KHT tumours were protected to a slightly lesser extent than were aerated tumours. For the KHT tumour, the number of clonogenic cells recovered from non-irradiated tumours one hour after DL-152 injection was reduced to 60 per cent of the number covered fro saline-injected controls, while, if DL-152 injected mice were acutely hypoxic at the time of sacrifice, the number of clonogenic cells was further reduced. The survival of non-irradiated EMT6 tumour cells was unaffected by DL-152 injection prior to sacrifice.

show abstract

“…Plummer et al (14) and Orlans et al (15) reported that the low doses of syrosin gopine which exhibited no inhibitory effect on conditioned avoidance response caused norepinephrine depletion in the heart and, therefore, syrosingopine appeared to cause a fall in blood pressure by depleting catecholamines in the peripheral tissues. Garattini et al (16) suggested that the fall in blood pressure caused by reserpine and bietaserpine could be correlated with the norepinephrine level in the heart. Furthermore, the central actions of CD-3400 such as a tranquillization, hypothermia or hypnosis and the depletion of serotonin level in the brain were weaker than those of rescinnamine and reserpine (17).…”

Section: Resultsmentioning

confidence: 99%

Antihypertensive Activity of Orally Administered Methyl O-(4-Hydroxy-3-Methoxycinnamoyl) Reserpate (CD-3400) in Conscious Hypertensive Rats

Kato

Nakao

Takagi

et al. 1977

Japanese Journal of Pharmacology

View full text Add to dashboard Cite

Abstract-Antihypertensive activity of orally administered methyl O-(4-hydroxy-3 methoxycinnamoyl)reserpate (CD-3400) was examined and compared with such activity of reserpine and its related agents in conscious hypertensive rats. CD-3400, 4-16 mg/kg p.o., produced a marked antihypertensive effect lasting 6 hr and a slight decrease in heart rate in spontaneously hypertensive rats (SHR). Reserpine, 1-4 mg/kg, rescin namine, 4-16 mg/kg, and syrosingopine, 8-32 mg kg p.o., produced effects similar to those of CD-3400. The order of antihypertensive activities of the agents was as follows: reserpine CD-3400-rescinnamine-_>syrosingopine.In renal hypertensive rats and deoxycorticosterone hypertensive rats, CD-3400 and rescinnamine, 4-16 mg/kg, and reserpine, 1-4 mg!kg p.o., also produced an antihypertensive effect and the order of potency was as follows: reserpine,~rescinnamine>CD-3400.Repeated adminis trations of CD-3400, 2-12 mg, kg;'day p.o., for 14 days, to SHR produced the marked constant antihypertensive effects during the administration period. The order of the potency was as follows: reserpine'; rescinnamine>CD-3400.CD-3400 possessing a sustained antihypertensive activity may be prescribed in cases when long-term therapy is required for hypertensive patients.Reserpine, one of the Rauwolfia alkaloids, has been used as an antihypertensive agent.Rescinnamine, which has a weaker activity than reserpine on the sympathetic nervous system, has been also extensively used for long-term treatment of hypertensive patients.Methyl O-(4-hydroxy-3-methoxycinnamoyl)reserpate (CD-3400) was originally de veloped by Kametani et al.(1) during a search for new derivatives without adverse effects such as mental depression, peptic ulcer, diarrhea and ptosis, and was found to possess a more potent antihypertensive activity than rescinnamine in spontaneously hypertensive rats when administered i.v. (1).In the present study, antihypertensive activities of orally administered CD-3400 in conscious hypertensive rats were examined and compared with those of reserpine and its related agents. MATERIALS AND METHODSBlood pressure and heart rate measurements in spontaneously hypertensive ratsBlood pressure and heart rate of spontaneously hypertensive rats (SHR) were measured

show abstract

Pharmacological and Biochemical Effects of Some Reserpine Derivatives

Cited by 18 publications

References 2 publications

The Effect of Reserpine, 5-Hydroxytryptamine and Other Drugs on Induced Ovulation in Immature Mice

The Effect of Reserpine, 5-Hydroxytryptamine and Other Drugs on Induced Ovulation in Immature Mice

Radioprotection of Normal and Malignant Tissue in the Mouse by Diethylaminoreserpine

Antihypertensive Activity of Orally Administered Methyl O-(4-Hydroxy-3-Methoxycinnamoyl) Reserpate (CD-3400) in Conscious Hypertensive Rats

Contact Info

Product

Resources

About