Each PDE have isogenies (PDE 4A, PDE 4B, PDE 4C, and PDE 4D), which had different level in tissues. A cell can contain one or more DPE type. When agent (or drug) specifically and inhibited isoenzym, it will have specific effect on proteinkinase. The PDE4 and PDE3/4 compound inhibitive drugs have effects at the same time to relax trachea and anti-inflammatory. Viagra is PDE5 selective inhibitor, more important than PDE 2-3-4 with 1000 times, PDE 1 with 80 times, PDE 6 and PDE 7 with 10 times. This agent have many in vessels and cavernosum corpus. It plays role of break dow GMPv, but it depends on NO.
Pharmaceutical Preparations ; antagonists & inhibitors

Histamine H1 Antagonists ; pharmacology ; Humans

No abstract available.
Antitussive Agents* ; Expectorants* ; Histamine Antagonists*

Chlopheniramine (chlorphenamine) is a racemic antiallergic antihistaminic H1 drug presenting 2 enantioners. The bioequivalence of two sustained-released formulations of racemic chlopheniramine combined with phenylpropanolamine was assessed firstly, in a dissolution test in vitro according to USP requirements. The present work compares in vitro dissolution rates of two formulations of chlopheniramine maleate. The two formulations are equivalent in vitro, both in a water medium or in a SGF/SIF medium. The pH is not a critical parameter affecting drug release and allows to use purified water for chlopheniramine dissolution test
Chlorpheniramine ; Pharmaceutical Preparations ; Histamine H1 Antagonists

Background: In Viet Nam, there were many researches on determining lead level in blood, food and environment. But until now, there were not researches on determining lead level in fishermen community. Objectives: Determine trace amount of lead by von-ampe dissolve anot using electrode BiFE. Analysis on trace amount of lead in blood and urine of fishermen in Canh Duong village. Propose solutions for preventing lead poisoning in studied community. Subjects and method: Fishermen in Canh Duong village, Phu Loc, Thua Thien Hue province. The method differential pulse-anodic stripping voltametry (DP-ASV) using Bismuth Film Electrodic in situ was successfully applied to measure lead levels in blood and 24h urine of fishermen in Canh Duong village. Results: The mean level of lead in blood of the suspected group (fishermen) in Canh Duong village (34,7 \xb5g/dL) was higher than that of the control group (16,3 \xb5g/dL). For both groups, 37 out of 40 blood samples (92,5%) had lead level higher than WHO\u2019s recommended level (10 \xb5g/dL). Especially, 6 of 40 blood samples (15%) had lead level higher than 50 \xb5g/dL. The lead level in 24h urine of suspected group had slightly higher (about 1,2 times) than that in the control group. The lead level of the two groups was much higher than the normal level. Conclusion: The method DP-ASV/BiFE in situ was applied successfully to determine lead level in blood and 24h urine. The investigative results of related information showed that: the risk of chronic lead poisoning in studied community very high.
Lead/ adverse effects ; chemistry ; antagonists & ; inhibitors ;

Adrenergic beta-Antagonists ; Arrhythmias, Cardiac ; Humans

AMD3100 (Plerixafor) is an antagonist of CXCR4, receptor for stromal cell-derived factor-1 (SDF-1).It disrupts binding of SDF-1 to CXCR4 by competing binding site, thus blocking the physiological function of SDF-1/CXCR4 axis. SDF-1/CXCR4 axis has been shown to play critical roles in stem cell mobilization, migration and homing, and in immunoregulation, inflammatory disease, autoimmune disorder, embryonic development, and tumor cell proliferation, migration and location. AMD3100 has been confined effective for the mobilization of HSC and MSC, inhibition of carcinoma growth and metastasis, suppression of some inflammatory and autoimmune disorder. Therefore, further research on AMD3100 will be helpful to understand the effects of bone marrow microenvironment on the pathogenesis of neoplasm, and to restore the traumatic tissues by mobilizing HSC effectively, that might provide a new idea and measure for the treatment of certain neoplasms. Some research progress of basic research and application on AMD3100 are summarized in this review.
Heterocyclic Compounds ; pharmacology ; Receptors, CXCR4 ; antagonists & inhibitors

Adrenergic beta-Antagonists ; therapeutic use ; Genomics

This study was undertaken to observe the effects of centrally administred antihistamines on the blood pressure. Diphenhydramine(DPH), a H1-receptor antagonist, and ranitidine(RAN), a H2-receptor antagonist were administered intracerebroventricularly(icv) on urethane-anesthetized rabbits. 1) Both DPH and RAN administered intraccebroventricularly increased blood pressure, however the intravenous(iv) adminstration of them did not affect blood pressure. The pressor response to icv DPH was dose-dependent, but that to icv RAN was not. 2) The pressor response to icv DPH(1mg) was either markedly attenuated or reversed to depressor response by the pretreatment with icv phentolamine(250,500ug), and iv chlorisondamine(0.1, 1mg/Kg) and iv phenoxybenzamine(1mg/Kg). In cord-sectioned rabbtis, icv RAN) 1mg) did not produce pressor response. 3) The pressor responsr to icv RAN(1mg) was not affected by the pretreatment with icv phentolamine(500ug), iv chlorisondamin(1mg/Kg) and iv phenoxybenzamine(1mg/Kg), and iv phenoxybenzamine(1mg/Kg). RAN also producted pressor response in cordsectioned rabbits. These results suggest that the pressor response to icv DPH is elecited by increasing peripheral sympathetic tone via the stimulation of central alpha-adrenoreceptors and the pressor response to icv RAN is produced by releasing some humoral facotr which can increase blood pressure.
Blood Pressure ; Diphenhydramine* ; Histamine Antagonists ; Rabbits* ; Ranitidine*

PURPOSE: Medical therapy with an alpha-blocker is commonly used primarily in patients with benign prostatic hyperplasia (BPH). However, the efficacy of the alpha-blocker is still questionable in reference to a small prostate, with the size of 30g or less. We reviewed 117 patients who had been taken the alpha-blocker for the management of BPH, and the results were analyzed according to the prostatic size. MATERIALS AND METHODS: One hundred seventeen patients were divided into the two following groups: Group I consisted of 57 patients with a BPH of under 30g and Group II consisted of 60 patients with a BPH of over 30g. Both groups were evaluated for the international prostate symptom score, urine flow rate, and residual urine volume before and 3 months after receiving medical therapy with tamsulosin. RESULTS: The success rate after medical therapy was similar in both groups, and all components were significantly improved after 3 months. The improvement rate of the urine flow rate was more significant in group II than group I. CONCLUSIONS: According to several objective results and the preference of patients for this treatment, medical therapy with the alpha-blocker could be also available in patients with BPH of under 30g.
Adrenergic alpha-Antagonists ; Humans ; Prostate ; Prostatic Hyperplasia*