Detail of "17650-98-5"

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Histamine H2-receptor agonists and antagonists on pancreatic exocrine secretion of the dog

Histamine H2-receptor agonists and antagonists on pancreatic exocrine secretion of the dog. Bertaccini, G.; Coruzzi, G. (Sch. Med., Univ. Parma, Parma 43100, Italy). Agents Actions, 16(3-4), 211-14 (English) 1985. CODEN: AGACBH. ISSN: 0065-4299. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) Section cross-reference(s): 1 The use of H2-receptor agonists and antagonists revealed that histamine [51-45-6] H2-receptors are present in pancreatic exocrine tissue and that their stimulation caused a dose-dependent increase in pancreatic juice. The fact that H2-antagonists and aminoguanidine [79-17-4] were unable to modify basal levels of pancreatic secretion seemed to minimize a role for H2-receptors in the regulation of pancreatic secretion. On the other hand H2-antagonists modified ceruletide [17650-98-5]-induced secretion in different ways according to the different mols. Ranitidine [66357-35-5] strongly potentiated, whereas cimetidine [51481-61-9], oxmetidine [72830-39-8], and mifentidine [83184-43-4] slightly inhibited, the effect of ceruletide. The stimulatory effect of eserine [57-47-6] and the inhibitory effect of atropine indicated a cholinergic interference in the action of ceruletide. Therefore, the potentiating effect of ranitidine may be related to its cholinomimetic action and the inhibitory effect of the other H2-antagonists may be connected with an anticholinergic effect. However, the potentiating effect of aminoguanidine on ceruletide-induced secretion may indicate a possible role for histamine in the response to ceruletide.

Modulation of rat pancreatic muscarinic cholinergic receptors by caerulein

Modulation of rat pancreatic muscarinic cholinergic receptors by caerulein. Delhaye, Myriam; Taton, Gerard; Poirier, Guy; Larose, Louise; St-James, Sylvie; Morisset, Jean (Med. Surg. Dep. Gastroenterol., Erasme Hosp., Brussels B-1070, Belg.). Biochem. Pharmacol., 34(7), 1057-63 (English) 1985. CODEN: BCPCA6. ISSN: 0006-2952. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) To evaluate the modulation of pancreatic muscarinic receptors in 2 states of pancreatic growth, hypertrophy and hyperplasia, caerulein [17650-98-5] (1 mg/kg) was administered 3 times daily for 2 and 4 days to adult rats. After 2 days of treatment, pancreatic hypertrophy was well established as evidenced by increases in pancreatic wt., cellular mass, and protein content. Using an increase in DNA content as an index of hyperplasia, pancreatic hyperplasia occurred only after 4 days of caerulein treatment. Caerulein increased the concn. of muscarinic receptors per DNA in pancreatic homogenate by 57% over the control value after 2 days of treatment without modification of the receptor affinity for the ligand, quinuclidinyl benzilate. This increase involved mainly receptors in the low-affinity state for carbamylcholine [462-58-8] and their concn. returned to control levels after 4 days of treatment. The functional capacity of the acini increased after 2 days of caerulein as amylase release increased, but the sensitivity of these acini to carbamylcholine decreased. After 4 days of caerulein, the functional capacity returned towards control values but the sensitivity to carbamylcholine remained decreased. The increase in muscarinic receptor concn. could be ascribed to a general increase in cellular proteins, as part of the hypertrophic effect of caerulein. This specific effect would also explain the increased functional secretory capacity of the caerulein-treated acini, but the decreased sensitivity to carbamylcholine probably resulted in changes at a postreceptor locus, since the affinities of the muscarinic receptors for carbamylcholine remained unaffected.