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Metabolism: Clinical and Experimental Apr 1982Betazole, a pyrazole analogue of histamine, as well as pentagastrin and HCl stimulate GIP secretion. We have asked the question as to whether betazole acts directly or...
Betazole, a pyrazole analogue of histamine, as well as pentagastrin and HCl stimulate GIP secretion. We have asked the question as to whether betazole acts directly or via the production of HCl. Eight normal subjects and 4 patients with achlorhydria secondary to pernicious anemia were given betazole (0.5 mg/kg) by IM injection. Another six normal subjects were also given betazole but this was preceded by 200 mgs. of the H2 receptor blocker cimetidine given IV 60 mins. previously and a slow infusion of 200 mg. cimetidine given over the next 4 hr. Our results have shown that the GIP response to betazole is maintained in achlorhydric subjects as well as during H2 blockade. The results suggest that betazole and therefore histamine may stimulate GIP directly and not necessarily via the mediation of HCl.
Topics: Achlorhydria; Adolescent; Adult; Anemia, Pernicious; Betazole; Blood Pressure; Cimetidine; Gastric Acid; Gastric Inhibitory Polypeptide; Gastritis, Atrophic; Gastrointestinal Hormones; Humans; Male; Middle Aged; Pyrazoles; Time Factors
PubMed: 7078422
DOI: 10.1016/0026-0495(82)90114-7 -
Green Chemistry : An International... May 2021As an alternative to classical synthetic approaches for the production of betazole drug, a one-pot biocatalytic system for this pharmaceutical molecule from its alcohol...
As an alternative to classical synthetic approaches for the production of betazole drug, a one-pot biocatalytic system for this pharmaceutical molecule from its alcohol precursor has been developed. An ω-transaminase, an alcohol dehydrogenase and a water-forming NADH oxidase for cofactor recycling have been combined to catalyse this reaction, yielding 75% molar conversion in batch reactions with soluble enzymes. This multienzyme system was then co-immobilised through a newly established protocol for sequential functionalization of a methacrylate-based porous carrier to enable tailored immobilisation chemistries for each enzyme. This pluri-catalytic system has been set up in a continuous flow packed-bed reactor, generating a space-time yield of up to 2.59 g L h with 15 min residence and a constant supply of oxygen for cofactor recycling through a segmented air-liquid flow. The addition of an in-line catch-and-release column afforded >80% product recovery.
PubMed: 34220333
DOI: 10.1039/d1gc01095f -
Journal of the American Medical... Jun 1956
Topics: Adrenocorticotropic Hormone; Betazole; Histamine; Humans
PubMed: 13318941
DOI: No ID Found -
Gastroenterologia Japonica Apr 1986The effects of dibutyryl cyclic AMP (db-cAMP), dibutyryl cyclic GMP (db-cGMP), betazole hydrochloride (betazole) and acetylcholine (ach.) on pepsinogen secretion from...
The effects of dibutyryl cyclic AMP (db-cAMP), dibutyryl cyclic GMP (db-cGMP), betazole hydrochloride (betazole) and acetylcholine (ach.) on pepsinogen secretion from isolated rabbit gastric mucosa were studied using an organ culture system. The 10(-3) M db-cAMP, but not db-cGMP of any concentration, produced a significant enhancement of pepsinogen secretion into the culture medium. In the presence of aminophylline (phosphodiesterase inhibitor), betazole stimulated pepsinogen secretion at concentrations of 10(-8), 10(-6) and 10(-4) M. The 10(-4) M betazole stimulated pepsinogen secretion most strongly (208% of control) and 10(-6) M betazole induced submaximal secretion (137% of control). Ach. stimulated pepsinogen secretion at 10(-8), 10(-6), 10(-4) and 10(-2) M. The peak secretion occurred at 10(-4) M ach. (303% of control). Betazole (with aminophylline) against a background of 10(-6) M ach. (submaximal stimulation dose), produced an intense stimulation of pepsinogen secretion at the concentrations of 10(-8), 10(-6) and 10(-4) M, and the secretion rate expressed as percent of control were 277, 350 and 329%, respectively. These responses were not considered the additive action by betazole and ach. but the potential interaction between the two agents in pepsinogen secretion. From these findings, we conclude that betazole-ach. interdependency exists in in vitro pepsinogen secretion.
Topics: Acetylcholine; Animals; Betazole; Bucladesine; Dibutyryl Cyclic GMP; Drug Interactions; Gastric Mucosa; Nucleotides, Cyclic; Organ Culture Techniques; Pepsinogens; Pyrazoles; Rats; Secretory Rate
PubMed: 3011576
DOI: 10.1007/BF02774830 -
Digestion 1982The effects of betazole hydrochloride, dibutyryl cyclic AMP (DB-cyclic AMP) and betazole hydrochloride plus aminophylline on pepsinogen secretion by rabbit gastric...
The effects of betazole hydrochloride, dibutyryl cyclic AMP (DB-cyclic AMP) and betazole hydrochloride plus aminophylline on pepsinogen secretion by rabbit gastric mucosa were studied in organ culture. Betazole hydrochloride alone did not stimulate pepsinogen secretion at the concentrations of 10(-8), 10(-6), 10(-5) and 10(-4) M. However, 10(-3) M DB-cyclic AMP produced a significant stimulation of pepsinogen secretion into the culture medium when compared with the control. In the presence of 3 x 10(-3) M aminophylline, betazole hydrochloride in the concentration of 10(-5) and 10(-4) M stimulated pepsinogen secretion into the culture medium, and the magnitude of this increase was 2.0- and 2.8-fold, respectively, compared with the control. Aminophylline alone could not change pepsinogen secretion into the culture medium. These results suggested that the pepsinogen secretion, stimulated by betazole hydrochloride, was mediated by cyclic AMP in the chief cells.
Topics: Aminophylline; Animals; Betazole; Bucladesine; Cyclic AMP; Gastric Mucosa; Organ Culture Techniques; Pepsinogens; Pyrazoles; Rabbits; Stimulation, Chemical
PubMed: 6286392
DOI: 10.1159/000198724 -
Gastroenterology May 1977A significant association has previously been found between a betazole-induced decrease in serum group I pepsinogen (PG I) levels and a low peak acid output (PAO) in... (Comparative Study)
Comparative Study
A significant association has previously been found between a betazole-induced decrease in serum group I pepsinogen (PG I) levels and a low peak acid output (PAO) in symptomatic patients with vagotomy and gastric resection or a drainage procedure. This study compares the effect of betazole on serum PG I levels and gastric acid output in 245 unoperated patients (115 duodenal ulcer, 25 prepyloric ulcer, 32 gastric ulcer, 73 nonulcer) and in 73 symptomatic postoperative patients (15 subtotal gastric resection, 28 vagotomy and gastric resection, 30 vagotomy and drainage). A negative serum PGI response (2-hr serum PG I level less than 92% of basal) occurred in 10 (4.1% of the unoperated patients and in 31 (42.5%) of the postoperative patients. Seven (70%) of the former and 29 (93.5%) of the latter patients had a PAO of less than 10 mEq per hr, indicating that a negative serum PG I response is associated with a low PAO in both unoperated and postoperative patients. The PAO was greater than 10 mEq per hr in 93.1% of the 277 patients with a 2-hr serum PG I level of more than 92% of basal. Additional studies revealed that neither aspiration of gastric juice nor perfusion of the stomach with acid altered the serum PG I response. This suggests that topical acid does not modulate the effect of betazole on serum PG I levels. Finally, a negative serum PG I response has been shown to be paradoxical, in that gastric pepsin levels have been found to increase over basal concurrently with the decrease in serum PG I levels.
Topics: Betazole; Gastrectomy; Gastric Juice; Gastric Mucosa; Humans; Pepsinogens; Peptic Ulcer; Postoperative Care; Pyrazoles; Stomach; Time Factors; Vagotomy
PubMed: 849814
DOI: No ID Found -
Molecules (Basel, Switzerland) Jan 2018Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of... (Review)
Review
Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.
Topics: Animals; Anti-HIV Agents; Anti-Inflammatory Agents; Anti-Obesity Agents; Antidepressive Agents; Antipsychotic Agents; Chemistry, Pharmaceutical; Drug Design; Humans; Pyrazoles
PubMed: 29329257
DOI: 10.3390/molecules23010134 -
Scandinavian Journal of Gastroenterology Oct 1986The effect of omeprazole, given as a buffered solution, on basal acid secretion and that induced by betazole and sham feeding in healthy subjects were studied. The three... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
The effect of omeprazole, given as a buffered solution, on basal acid secretion and that induced by betazole and sham feeding in healthy subjects were studied. The three series of experiments showed a dose-dependent acid reduction during the 2nd to 4th h after administration of omeprazole in doses of 10-60 mg, with almost complete inhibition by the highest dose. The ED50 values were of the same magnitude for basal and stimulated acid secretion. This indicates that omeprazole is an equally potent inhibitor of both kinds of acid secretion irrespective of the manner in which the acid is activated.
Topics: Adult; Betazole; Dose-Response Relationship, Drug; Food; Gastric Acid; Humans; Male; Omeprazole; Pyrazoles; Stomach
PubMed: 3775255
DOI: 10.3109/00365528608996412 -
The Medical Letter on Drugs and... Jul 1975
Topics: Betazole; Gastric Acidity Determination; Gastrins; Histamine; Humans; Injections, Subcutaneous; Pentagastrin; Radioimmunoassay
PubMed: 1134447
DOI: No ID Found -
JAMA May 1961
Topics: Betazole; Central Nervous System Stimulants; Gastric Juice; Histamine; Humans; Stomach
PubMed: 14448724
DOI: 10.1001/jama.1961.63040100023020b