Betazole
(Synonyms: 倍他唑,Ametazole) 目录号 : GC61539Betazole Dihydrochloride (Ametazole, 2-(3-Pyrazolyl)ethanamine) is a histamine H2 agonist used clinically to test gastric secretory function.
Cas No.:105-20-4
Sample solution is provided at 25 µL, 10mM.
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Betazole Dihydrochloride (Ametazole, 2-(3-Pyrazolyl)ethanamine) is a histamine H2 agonist used clinically to test gastric secretory function.
Cas No. | 105-20-4 | SDF | |
别名 | 倍他唑,Ametazole | ||
Canonical SMILES | NCCC1=NNC=C1 | ||
分子式 | C5H9N3 | 分子量 | 111.15 |
溶解度 | DMSO: 250 mg/mL (2249.21 mM) | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg | |
1 mM | 8.9969 mL | 44.9843 mL | 89.9685 mL |
5 mM | 1.7994 mL | 8.9969 mL | 17.9937 mL |
10 mM | 0.8997 mL | 4.4984 mL | 8.9969 mL |
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2.
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Betazole-induced GIP secretion is not mediated by gastric HCl
Metabolism 1982 Apr;31(4):380-2.PMID:7078422DOI:10.1016/0026-0495(82)90114-7.
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.
Biocatalytic access to Betazole using a one-pot multienzymatic system in continuous flow
Green Chem 2021 May 24;23(12):4594-4603.PMID:34220333DOI:10.1039/d1gc01095f.
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 in situ 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-1 h-1 with 15 min residence and a constant supply of oxygen for in situ cofactor recycling through a segmented air-liquid flow. The addition of an in-line catch-and-release column afforded >80% product recovery.
Effects of Betazole hydrochloride and cyclic AMP on the pepsinogen secretion by rabbit gastric mucosa in organ culture
Digestion 1982;23(3):169-73.PMID:6286392DOI:10.1159/000198724.
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.
Effects of cyclic nucleotides, Betazole hydrochloride and acetylcholine on pepsinogen secretion from isolated rabbit gastric mucosa
Gastroenterol Jpn 1986 Apr;21(2):129-34.PMID:3011576DOI:10.1007/BF02774830.
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.
Inhibitory effect of bromazepam on basal and betazole-stimulated gastric acid secretion in man
Gut 1974 Feb;15(2):116-20.PMID:4820635DOI:10.1136/gut.15.2.116.
Basal, as well as betazole-stimulated gastric acid secretion in man is reduced after the intravenous administration of bromazepam. In subjects staying awake, this reduction is limited to the first two 15-minute periods. The reduction is highly significant in subjects who fall asleep after receiving the drug. Natural sleep causes the same depression. The low level of acid secretion is maintained until the subjects are awakened when there is a sharp and highly significant rise. Acid secretion in subjects who fall asleep after the simultaneous administration of Betazole and bromazepam is significantly higher than after the administration of bromazepam alone. Sleep causes a much greater depression of basal and betazole-stimulated acid secretion than does the benzodiazepine itself. Acid secretion was measured by continuous intragastric titration and a pH-sensitive endoradiosonde.