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1. |
Current views of zinc as a gastrohepatic protective agent |
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Drug Development Research,
Volume 17,
Issue 3,
1989,
Page 185-197
C. H. Cho,
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摘要:
AbstractThe protective effects of zinc on gastrohepatic lesions induced by various agents are reviewed. Acute gastric glandular mucosal damage produced by parenteral injection of reserpine, cold‐restraint stress or by oral administration of ethanol are prevented by zinc compounds. Hepatic lesions induced by CCl4, ethanol, alkylating agents, or cadmium are also antagonized by zinc ions. The pathological changes evoked by these agents or stress are postulated to be due to free radical production and labilization of biomembranes. These actions are thought to be sequestered or stabilized by zinc. The role of glutathione in the protective action and the involvement of mast cell degranulation in ulceration are further discussed. The data available so far indicate that zinc compounds could be used as protective agents for gastrohepatic disease
ISSN:0272-4391
DOI:10.1002/ddr.430170302
出版商:Wiley Subscription Services, Inc., A Wiley Company
年代:1989
数据来源: WILEY
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2. |
Pharmacologic modulation by cetirizine 2 HCl and loratadine of the histamine‐induced skin reaction in mice and in humans |
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Drug Development Research,
Volume 17,
Issue 3,
1989,
Page 199-206
P. Coulie,
C. De Vos,
L. Ghys,
J. P. Rihoux,
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摘要:
AbstractIn mice, the histamine‐induced cutaneous reaction is inhibited by cetirizine with an approached ED50of 0.04 mg/kg and by loratadine with an approached ED50of 0.38 mg/kg, both drugsadministered intraperitoneally. At these doses, cetirizine' s onset of activity seems to be more rapid, although both compounds show the same duration for at least 7 hr. Nine healthy volunteers received orally either cetirizine or loratadine (10 mg single dose) or placebo in a double‐blind randomized and cross‐over study design. Both drugswere significantly more effective than placebo (except loratadine at the 2nd and 24th hr for the wheal with 1 and 10 μg histamine, and at the 2nd hr for the flare with 1 μg histamine). At all times and withboth agonists' concentrations, cetirizine was significantly more potent than loratadine (except at the 24th hr for the wheal with 1 μghistamine). Neither numerous nor marked side effects we
ISSN:0272-4391
DOI:10.1002/ddr.430170303
出版商:Wiley Subscription Services, Inc., A Wiley Company
年代:1989
数据来源: WILEY
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3. |
Antihypertensive property of a novel uricosuric diuretic, S‐8666, in rats |
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Drug Development Research,
Volume 17,
Issue 3,
1989,
Page 207-217
Saburo Matsuda,
Mitsuo Ishii,
Naoko Kitajiri,
Isao Yahara,
Hiroshi Harada,
Yukio Yonetani,
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摘要:
AbstractThe antihypertensive, diuretic, and toxicological effects of S‐8666 were studied in rats. At doses of more than 60 mg/kg/day, p.o., S‐8666 was antihypertensive in DOCA‐salt hypertensive rats with a potency corresponding to 1/20 of that of trichlormethiazide. The antihypertensive effect was dose‐dependent, and, at the higher doses, S‐8666 had a more potent depressor effect than trichlormethiazide. The antihypertensive activity of S‐8666 was shown predominantly by the S‐(−)‐enantiomer, with the R‐(+)‐enantiomer being only slightly active. A similar dose‐dependent antihypertensive effect was shown by furosemide, tienilic acid, or indacrinone, but the therapeutic index (LD50/minimum effective dose) of S‐8666 was the highest among them. The acute diuretic and natriuretic effects of S‐8666 after oral administration of 60–200 mg/kg to DOCA‐salt hypertensive rats correlated well with its antihypertensive effect, although such diuretic and natriuretic effects in normotensive rats had no effect on blood pressure. S‐8666, like trichlormethiazide, showed a prophylactic effect on the development of hypertension in DOCA‐salt hypertensive rats, salt‐loaded spontaneously hypertensive rats (SHR), and salt‐loaded Dahl‐S rats, though it was much less potent. Moreover, the combination of S‐8666 with captopril in SHR enhanced the depressor effect of captopril like hydrochlorothiazide. These results indicate that S‐8666 can be an effective nonthiazide
ISSN:0272-4391
DOI:10.1002/ddr.430170304
出版商:Wiley Subscription Services, Inc., A Wiley Company
年代:1989
数据来源: WILEY
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4. |
Aspirin plasma monitoring in juvenile chronic arthritis |
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Drug Development Research,
Volume 17,
Issue 3,
1989,
Page 219-226
Bhawna Sharma,
Vimlesh Seth,
Shiva D. Seth,
Nandita Basu,
Alka Beotra,
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摘要:
AbstractThirty‐two patients from the Pediatric Rheumatology Clinic of the All India Institute of Medical Sciences, New Delhi, suffering from juvenile chronic arthritis (JCA) in the age group of 5–15 years were investigated for salicylate monitoring. Of these, 15 (46.9%) had polyarthritis and 11 (34.4%) suffered from systemic onset type of JCA while only 6 (18.7%) had the pauciarticular type of disease. Plasma salicylate and albumin levels were estimated on days 1, 7, 14, and 21, after initiation of therapy with aspirin. Serum SGOT and SGPT were also estimated, as well as clinical evidence of hepatotoxicity. The therapeutic plasma levels (15–25 mg/dl) of salicylates were achieved by a mean dose of aspirin of 81.8 mg/kg/day administered in three divided doses. On the surface area basis the mean dose of aspirin was 2.1 g/m2/day. Steady‐state level of aspirin in plasma was achieved by the seventh day, and the values were 2.8 times more than on the first day. In malnourished patients with low albumin levels, there was a proportional decrease in salicylate binding. Although increase in transaminase levels of 1 1/2 to 2 times the normal was observed in the patients on aspirin therapy, none of the children developed clinical evidence of hepatotoxicity during this short‐term study. The studies indicate that dosage of salicylates can be given either on a body weight or surface area basis. A malnourished child with lower levels of serum albumin may be more predisposed to salicylate toxicity, due to higher levels of free salicylates. There was no evidence of hepatotoxicity in the dosage range of 70–110 mg/kg/day or 1.9 to 2
ISSN:0272-4391
DOI:10.1002/ddr.430170305
出版商:Wiley Subscription Services, Inc., A Wiley Company
年代:1989
数据来源: WILEY
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5. |
Prevention of “learned helplessness” in the rat by hydroxyzine |
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Drug Development Research,
Volume 17,
Issue 3,
1989,
Page 227-236
Roger D. Porsolt,
Patrick Martin,
Antoine Lenégre,
Sylvie Fromage,
Corneliu E. Giurgea,
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摘要:
AbstractThe effects of hydroxyzine (8, 16, and 32 mg/kg i.p.), administered either 30 min before exposing rats to a series of inescapable shocks (preventive treatment) or during the subsequent acquisition of a shuttle box avoidance response (curative treatment), wereinvestigated. In these conditions untreated rats, previously exposed to inescapable shocks (“stress” ), show a marked increase in escape failures in the shuttle box when compared with nonshocked control animals (“ learned helplessness” ). Control experiments examined the effects of hydroxyzine on memory (passive avoidance test) and on electric shock sensitivity. Diazepam (2 mg/kg i.p.) was used as a reference compound. Hydroxyzine, when administered before “ stress,” clearly decreased at 8 and 32 mg/kg the number of escape failures observed but was without effect when administered after “stress” during the subsequent shuttle box avoidance learning. Similar results were observed with diazepam. Unlike diazepam, hydroxyzine at 32 mg/kg−1induced no amnesia in the passive avoidance test, whereas clear amnesia was observed with diazepam. Neither compound altered the rats' sensitivity to shock. These results suggest that hydroxyzine decreases the effects of “ stress” and that these effects cannot be attributed either to impaired memory for the aversive stimulation or to diminis
ISSN:0272-4391
DOI:10.1002/ddr.430170306
出版商:Wiley Subscription Services, Inc., A Wiley Company
年代:1989
数据来源: WILEY
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6. |
Pentylenetetrazol discriminative stimuli are selective for identifying benzodiazepine receptor modulating agents |
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Drug Development Research,
Volume 17,
Issue 3,
1989,
Page 237-243
Douglas E. Wilson,
Debra A. Bennett,
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摘要:
AbstractPentylenetetrazol (PTZ) has been reported to produce a discriminative stimulus related to anxiety and antagonized by the classical anxiolytics. In the present investigation, a variety of compounds with either benzodiazepine (BZ)‐type anxiolytic actions or other novel mechanisms of action (serotonin andN‐methyl‐D‐aspartate [NMDA] antagonism) were tested for their ability to antagonize this stimulus. Compounds that have been shown to modulate benzodiazepine receptor function were active in blocking PTZ, the discriminative stimulus. The failure of the other compounds to block these stimuli suggests that the PTZ discrimination may be selective for substances that modulate, either directly or indirectly, the BZ receptor
ISSN:0272-4391
DOI:10.1002/ddr.430170307
出版商:Wiley Subscription Services, Inc., A Wiley Company
年代:1989
数据来源: WILEY
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7. |
Modification of ischemia‐induced biochemical changes in the myocardium by Rooh‐Afza extracts |
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Drug Development Research,
Volume 17,
Issue 3,
1989,
Page 245-252
Madhu Dikshit,
Ranjana Srivastava,
Rikhab Chand Srimal,
Bhola Nath Dhawan,
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摘要:
AbstractIn rats, myocardial ischemia was produced by isoprenaline (80 mg/kg i.p.) and in rabbits, by ligating the anterior descending branch of the coronary artery. Two extracts of Rooh‐Afza, a Unani polypharmaceutical preparation, were administered 1 hr or 15 min before inducing ischemia. Both the extracts protected the rat myocardium from isoprenaline‐induced changes. In rabbits, protection against ischemia was observed only at a higher dose. The extract containing essential oils and flavoring agents was found to be more effective. It also inhibited platelet aggregation induced by adenosine diphosphate (ADP) in vitro and ex vivo in monk
ISSN:0272-4391
DOI:10.1002/ddr.430170308
出版商:Wiley Subscription Services, Inc., A Wiley Company
年代:1989
数据来源: WILEY
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8. |
Masthead |
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Drug Development Research,
Volume 17,
Issue 3,
1989,
Page -
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ISSN:0272-4391
DOI:10.1002/ddr.430170301
出版商:Wiley Subscription Services, Inc., A Wiley Company
年代:1989
数据来源: WILEY
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