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Volume 11, Issue 2
Displaying 1-8 of 8 articles from this issue
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VICTOR A. DRILL1962 Volume 11 Issue 2 Pages 77-87
Published: March 01, 1962
Released on J-STAGE: February 09, 2007
JOURNAL FREE ACCESSThe possibility that a salt regulating hormone played a causative role in the production of edema was developed from the early reports of several investigators. Various authors were able to obtain urinary extracts with good sodium retaining effects from edematous patients with congestive heart failure, nephrosis, or cirrhosis of the liver (cf. 1-4). Simpson, Tait, and Bush (5) discovered the steroid aldosterone in 1952, and in 1954 the sodium retaining factor in the urine of edematous patients was identified as aldosterone by Luetscher and coworkers (6, 7).
In view of the probable role that aldosterone played in the production and maintenance of edema we then asked the question “Would compounds with an aldosterone-blocking activity be effective in relieving edema?”. There was an excellent chance that such a relationship would exist and experiments were begun in 1954 by Dr. C. M. Kagawa to study the effects of salt retaining steroids so as to reliably determine their effect. on electrolyte excretion in experimental animals. These investigations were followed by an evaluation of structurally related steroids to determine whether or not they would block the electrolyte effects of the mineralocorticoids. Such studies led to the development of new steroids, the spirolactones, which are capable of blocking the salt retaining effects of desoxycorticosterone and aldosterone in laboratory animals and of producing a diuresis in patients with edema. The properties of the spirolactones, particularly Aldactone, will be discussed.View full abstractDownload PDF (539K) -
VICTOR A. DRILL1962 Volume 11 Issue 2 Pages 88-100
Published: March 01, 1962
Released on J-STAGE: February 09, 2007
JOURNAL FREE ACCESSOvulation is physiologically inhibited during pregnancy. The ovarian hormones produced by the corpus luteum of pregnancy, and later by the placenta, are responsible for this effect. Similarly, the administration of the naturally occurring steroids, such as estradiol and progesterone can inhibit ovulation. However, these steroids are unsatisfactory for clinical use as they are not regularly effective and secondly, the parenteral administration of progesterone is painful. The male hormone, testosterone, can also inhibit ovulation but cannot be used routinely clinically because of androgenic side effects. Thus, a search of other steroid derivatives was undertaken in attempts to find a satisfactory compound for human use.View full abstractDownload PDF (698K) -
HAJIME FUJIMURA, NORIO SUGIMOTO, GORO HAYASHI1962 Volume 11 Issue 2 Pages 101-113
Published: March 01, 1962
Released on J-STAGE: February 09, 2007
JOURNAL FREE ACCESSThe structure-activity relationship of various chemical compounds, which resembled to morphine in their structures and were synthesized by Sugimoto et al. (1), has been reported. Among those compounds a racemic 6-hydroxy-4a, 10-trimethylene-1, 2, 3, 4, 4a, 9, 10, 10a-octahydrophenanthridine hydrochloride (DH-7), which have a nitrogen atom at 9-position of the morphinan ring, showed almost the same strong analgesic activities as morphine hydrochloride in a series of screening test.
Further studies of the analgesic activity of DH-7 and the comparative pharmacological studies of the drug with morphine hydrochloride and levorphanol tartrate are described in this report. DH-7 has a chemical structure, shown in the following structural formula.View full abstractDownload PDF (517K) -
MANABU YASUDA1962 Volume 11 Issue 2 Pages 114-125
Published: March 01, 1962
Released on J-STAGE: February 09, 2007
JOURNAL FREE ACCESSAlthough there are many reports as to the hypothermic effect of reserpine (1-5), the exact mechanism of this action appears to be undecided. Recently, the action of reserpine has been found to be associated with the depletion of 5-hydroxytryptamine (5-HT) or catecholamine in the brain and the direct action of the alkaloid itself would be, if any, fairly negligible (6-12). After monoamine oxidase inhibitors had been introduced to pharmacology their effects were also studied on the reserpine action by many authors (13-20). Tyramine is known to have a pyrogenic action. Bachtold and Pletscher (21) demonstrated that rabbits pretreated with iproniazid exhibited a marked hyperthermia by the subsequently administered tyramine, phenylethylamine, 5-HT or reserpine. Horita (22) and Horita and Gogerty (23) showed that the pyrogenic activity of 5-hydroxytryptophane, a possible precursor of 5-HT, was greatly enhanced by pretreatment with either iproniazid or beta-phenylisopropylhydrazine (PIH). In addition, Horita (22) has found that preliminary treatment of rabbits with PIH produced a marked excitation and hyperthermia with subsequent administration of reserpine. Such “reserpine reversal” was also observed between iproniazid and reserpine except in a few cases (19-21, 23).
Kroneberg et al. (24) have shown that the pyrogenic effect of E. coli lipopolysaccharide (LPS), purified by the method of Westphal et al. (25) is inhibited by pretreatment with reserpine and that the fever thus inhibited reappeared when iproniazid is given. Going (26) has confirmed this finding and has reported the augmentation of febrile responses of animals to bacterial pyrogens by pretreatment with iproniazid.
These interesting results may indicate that biogenic amines such as 5-HT or catecholamines could play an important role in the pyrogenic activity of bacterial pyrogens. The question remains whether the bacterial endotoxins injected intravenously in animals gain access to the brain by crossing the blood-brain barrier or it is possible that the bacterial endotoxin may not have a direct action on the thermoregulatory center, and that the active principle transferrable across the blood-brain barrier may be some of the products, derived from bacterial endotoxins. Another possibility involves a substance in the animal body produced secondarily to the effect of bacterial pyrogens. This, in substance, covers the two theories on pyrogenic effects of bacterial pyrogens, i.e., ‘endogenous pyrogen’ (27-31) and ‘endogenous serum pyrogen’ (32-34).
The present paper deals with a study of the possible relationship between the biogenic amine and the pyrogenic effects of several substances, bacterial as well as chemical in origin. An attempt was also made to elucidate whether these substances cross the bloodbrain barrier and whether they have a direct effect on the thermoregulatory center in brain or not.View full abstractDownload PDF (553K) -
NOBORU TODA1962 Volume 11 Issue 2 Pages 126-140
Published: March 01, 1962
Released on J-STAGE: February 09, 2007
JOURNAL FREE ACCESSIn the course of studies in this laboratory on the mode of action of catecholamines on the transmembrane potential of the extirpated atrium of rabbit (1), some of the potentials recorded from the pacemaker area (West) responded differently to reserpine and adrenaline from the typical pacemaker potentials. The potential under this study was recorded from the area which was somewhat wider than the triangular pacemaker area shown schematically by West (2). This potential was characteristic in a notching of the upstroke and a slow rate of depolarization, and was very sensitive to reserpine and adrenaline. The notched potential in the sinoatrial node of rabbit's heart was at first reported by West (2), who studied the distribution of the potential. Although the similar notched potentials have been reported in the atrioventricular node of mammalian heart (3, 4), the smooth muscle of uterus (5) and the sinoauricular funnel of amphibian heart (6), the exact nature of the potentials remains to be settled. In the present report the responses of the notched potential recorded from the sinoatrial node of rabbit's heart were studied. It is expected that the responses of the potential to reserpine and adrenaline might have some contribution to elucidate the mechanism of the pacemaker activity.View full abstractDownload PDF (679K) -
KEIJI NAKAMURA, FREDERICK BERNHEIM1962 Volume 11 Issue 2 Pages 141-150
Published: March 01, 1962
Released on J-STAGE: February 09, 2007
JOURNAL FREE ACCESSLittle work has been done to identify the chemical nature of Florey's I Factor which inhibits the stretch receptor discharge, since the compound was originally defined by Florey (1) in 1954.
The Factor I turns out to be several compounds, GABA3 and β-alanine (2), which are present in the central nervous system (3, 4), β-hydroxy GABA (5), GGBA (6) found in mammal brain (7) and BGPA (6). More several related compounds were found as natural constituents in central nervous system, GABA-Ch (8), carnosin (9) and homocarnosin (10).
Physiological role of all compounds under consideration is not yet known. Postsynaptic structures possess an enzyme system capable of inactivating the released transmitter and the neurons must contain an enzyme system of synthesizing the compound. The transaminase might be one of such enzyme system participated.
A rapid incorporation of 14C-α-ketoglutarate into the glutamate pool was noted in experiments with rat brain homogenates (11).
This work concerns the transaminase activity of the compounds having Florey's I Factor and physiological unknown substances present in central nervous system, and the effect produced by administration of some drugs on the enzyme activity.View full abstractDownload PDF (462K) -
TATSUO KIKUCHI1962 Volume 11 Issue 2 Pages 151-170
Published: March 01, 1962
Released on J-STAGE: February 09, 2007
JOURNAL FREE ACCESSThe release and the depletion of noradrenaline (1) and serotonin (2) in the central nervous system by the administration of reserpine have been already confirmed by many investigators. Brodie et al. (3-6) showed that the sedative effect of reserpine derived from the release and the depletion of serotonin in the central nervous system. Subsequently, they discussed the role of the serotonergic or Hess' trophotropic system on the activity of the central nervous system. Carlsson (7, 8), on the contrary, discussed the role of noradrenaline on the activity of the system from the antagonistic action of 3, 4-dihydroxyphenylalanine (DOPA), the precursor of noradrenaline, on the sedative effect of reserpine in mice. In his experiment the administration of 5-hydroxytryptophane, the precursor of serotonin, to the sedated animal induced by reserpine did not reveal the similar antagonistic effect. Electroencephalographically studying the effects of reserpine, serotonin, 5-hydroxytryptophane and DOPA in rabbit, Monnier and Tissot (9) concluded that serotonin and 5-hydroxytryptophane stimulated the intralaminal thalamic system and depressed the reticular ascending system, while noradrenaline and DOPA showed an opposite effect. Costa et al. (10) studied the normal content of serotonin and noradrenaline in rabbit's brain in relation to the encephalographic pattern of the animal. They concluded that 5-hydroxytryptophane affected EEG by direct action on the mesodiencephalic reticular formation, and that the amounts of serotonin and noradrenaline as well as the rate of synthesis of the amines in the brain after the injection of monoamine oxidase inhibitors were the determining factors for the pattern of EEG.
The effect of reserpine on EEG of an intact rabbit was studied in combination with the administration of methamphetamine in the previous paper (11). In this report the effects of beta-phenylisopropylhydrazine, DOPA, 5-hydroxytryptophane and reserpine on the electroencephalographic activity of the neocortex, the limbic system and the reticular activating system including the thalamocortical system were studied in rabbit.View full abstractDownload PDF (1047K) -
RUBEN D. BUNAG, EDWARD J. WALASZEK1962 Volume 11 Issue 2 Pages 171-198
Published: March 01, 1962
Released on J-STAGE: February 09, 2007
JOURNAL FREE ACCESSDownload PDF (1575K)
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