Histamine receptors rapidly desensitize without altering nerve-evoked contractions in murine urinary bladder smooth muscle was written by Jones, B. Malique;Mingin, Gerald C.;Tykocki, Nathan R.. And the article was included in American Journal of Physiology in 2022.Related Products of 83799-24-0 The following contents are mentioned in the article:
Histamine has been implicated in urinary bladder dysfunction as an inflammatory mediator driving sensory nerve hypersensitivity. However, the direct influence of histamine on smooth muscle has not been thoroughly investigated. We hypothesized that histamine directly contracts urinary bladder smooth muscle (UBSM) independent of effects on nerves. Single cell quant. RT-PCR determined that only histamine H1 and H2 receptors were expressed on UBSM cells. In isolated tissue bath experiments, histamine (200μM) caused a highly variable and rapidly desensitizing contraction that was completely abolished by the H1 receptor antagonist fexofenadine (5μM) and the Gq/11 inhibitor YM254890 (1μM). Neither the muscarinic receptor antagonist atropine (1μM), the Na+ channel blocker tetrodotoxin (1μM), nor the transient receptor potential vanilloid type 1 antagonist capsazepine (10μM) altered responses to histamine, suggesting that nerve activation was not involved. UBSM desensitization to histamine was not due to receptor internalization, as neither the cholesterol-depleting agent methyl-β-cyclodextrin (10 mM), the dynamin-mediated endocytosis inhibitor dynasore (100μM), nor the clathrin-mediated endocytosis inhibitor pitstop2 (15μM) augmented or prolonged histamine contractions. Buffer from desensitized tissues still contracted histamine-naive tissues, revealing that histamine was not metabolized. Prolonged exposure to histamine also had no effect on contractions due to elec. field stimulation, suggesting that both efferent nerve and UBSM excitability were unchanged. Together, these data suggest that histamine, although able to transiently contract UBSM, does not have a lasting effect on UBSM excitability or responses to efferent nerve input. Thus, any acute effects of histamine directly on UBSM contractility are unlikely to alter urinary bladder function. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Related Products of 83799-24-0).
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Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem