Polyamines pipertramine (PIP) and pipertramine amide (PIPAM), unlike prototype methoctramine, displayed a potent inotropic effect in guinea pig atria. While the inotropic effect of PIP may be rationalized, as previously suggested, through a direct activation of a Gi/o protein, PIPAM effects were possibly the result of multiple interactions. Besides a direct Gi/o protein activation, PIPAM activated also muscarinic M 2 receptors by interacting most likely with an allosteric site. Binding experiments in CHO cells, expressing human cloned muscarinic M 2 receptors, confirmed that both compounds were effective muscarinic ligands.
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Titolo: | Polyamines may modulate both G protein-coupled receptors and G proteins. |
Autori: | |
Data di pubblicazione: | 2004 |
Rivista: | |
Handle: | http://hdl.handle.net/11581/202245 |
Appare nelle tipologie: | Articolo |