FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2000504997> ?p ?o ?g. }

• W2000504997 abstract "G-protein-coupled receptors (GPCRs) are considered the most diverse and ubiquitous family of integral membrane proteins and play a pivotal role in many cellular signalling pathways. In any single neuron, GPCRs can be located both pre- and postsynaptically or exclusively in either domain. Generally, activation of the same receptor at its different locations can result in modulation of different target ion channels. Nevertheless, a common feature of GPCRs is that when persistently activated, responses decrease over time, owing to receptor desensitization. Although it might be assumed that GPCRs at all sites on the same neuron are subject to similar levels of desensitization, a recent study has provided compelling evidence that this is not the case.Wetherington and Lambert have now shown that one GPCR, the adenosine A1-receptor, desensitizes more rapidly at postsynaptic sites compared with presynaptic sites, even when located on the same neuron [1xDifferential desensitization of responses mediated by presynaptic and postsynaptic A1 adenosine receptors. Wetherington, J.P. and Lambert, N.A. J. Neurosci. 2002; 22: 1248–1255PubMedSee all References][1]. Whole-cell patch-clamp recordings were made from hippocampal neurons that had been cultured in isolation to promote formation of autapses (synapses made by neurons on themselves). Responses to adenosine-A1-receptor stimulation were evident postsynaptically as activation of inwardly rectifying K? (GIRK) channels, and presynaptically as modulation of excitatory postsynaptic currents (EPSCs) through inhibition of voltage-gated Ca2+ channels in the terminal. Thus, by applying adenosine-A1-receptor agonists for prolonged periods, the desensitization rates of pre- and postsynaptic responses could be elucidated in the same neuron. Remarkably, the postsynaptic receptors desensitized within two hours, whereas presynaptic responses were unchanged until 12 hours or more of agonist exposure. Moreover, although postsynaptic responses recovered over a matter of hours, presynaptic effects took up to two days to recover. These effects appeared not to reflect modification of either ion channels or G proteins, as GABAB-receptor-mediated responses (which are likely to use the same pathway) were unchanged. Additionally, these effects could not be ascribed to a large receptor reserve present at presynaptic, but not postsynaptic, sites.These elegant experiments indicate that the subcellular localization of a GPCR can influence the rate of receptor desensitization. GPCRs are prime targets for the development of therapeutic agents designed to either block or activate the receptors. Furthermore, tolerance to, and dependence on, some addictive drugs has been strongly linked to chronic activation of GPCRs. Therefore, assuming this situation applies in more intact preparations, we might gain valuable insights into the cellular mechanisms underlying the differential development of tolerance to separate effects of the same drug." @default.
• W2000504997 created "2016-06-24" @default.
• W2000504997 creator A5028412248 @default.
• W2000504997 date "2002-06-01" @default.
• W2000504997 modified "2023-09-24" @default.
• W2000504997 title "Postsynaptic adenosine A1-receptors are the sensitive type" @default.
• W2000504997 cites W2134715486 @default.
• W2000504997 doi "https://doi.org/10.1016/s0166-2236(02)02178-1" @default.
• W2000504997 hasPublicationYear "2002" @default.
• W2000504997 type Work @default.
• W2000504997 sameAs 2000504997 @default.
• W2000504997 citedByCount "0" @default.
• W2000504997 crossrefType "journal-article" @default.
• W2000504997 hasAuthorship W2000504997A5028412248 @default.
• W2000504997 hasConcept C112592302 @default.
• W2000504997 hasConcept C134018914 @default.
• W2000504997 hasConcept C135285700 @default.
• W2000504997 hasConcept C142652207 @default.
• W2000504997 hasConcept C169760540 @default.
• W2000504997 hasConcept C170493617 @default.
• W2000504997 hasConcept C17077164 @default.
• W2000504997 hasConcept C182683403 @default.
• W2000504997 hasConcept C185592680 @default.
• W2000504997 hasConcept C197341189 @default.
• W2000504997 hasConcept C2776991684 @default.
• W2000504997 hasConcept C2778938600 @default.
• W2000504997 hasConcept C2779779143 @default.
• W2000504997 hasConcept C2910581834 @default.
• W2000504997 hasConcept C55493867 @default.
• W2000504997 hasConcept C67907053 @default.
• W2000504997 hasConcept C80631254 @default.
• W2000504997 hasConcept C86803240 @default.
• W2000504997 hasConcept C95444343 @default.
• W2000504997 hasConceptScore W2000504997C112592302 @default.
• W2000504997 hasConceptScore W2000504997C134018914 @default.
• W2000504997 hasConceptScore W2000504997C135285700 @default.
• W2000504997 hasConceptScore W2000504997C142652207 @default.
• W2000504997 hasConceptScore W2000504997C169760540 @default.
• W2000504997 hasConceptScore W2000504997C170493617 @default.
• W2000504997 hasConceptScore W2000504997C17077164 @default.
• W2000504997 hasConceptScore W2000504997C182683403 @default.
• W2000504997 hasConceptScore W2000504997C185592680 @default.
• W2000504997 hasConceptScore W2000504997C197341189 @default.
• W2000504997 hasConceptScore W2000504997C2776991684 @default.
• W2000504997 hasConceptScore W2000504997C2778938600 @default.
• W2000504997 hasConceptScore W2000504997C2779779143 @default.
• W2000504997 hasConceptScore W2000504997C2910581834 @default.
• W2000504997 hasConceptScore W2000504997C55493867 @default.
• W2000504997 hasConceptScore W2000504997C67907053 @default.
• W2000504997 hasConceptScore W2000504997C80631254 @default.
• W2000504997 hasConceptScore W2000504997C86803240 @default.
• W2000504997 hasConceptScore W2000504997C95444343 @default.
• W2000504997 hasLocation W20005049971 @default.
• W2000504997 hasOpenAccess W2000504997 @default.
• W2000504997 hasPrimaryLocation W20005049971 @default.
• W2000504997 hasRelatedWork W1493378289 @default.
• W2000504997 hasRelatedWork W1595326866 @default.
• W2000504997 hasRelatedWork W1608872832 @default.
• W2000504997 hasRelatedWork W1963526287 @default.
• W2000504997 hasRelatedWork W1964655580 @default.
• W2000504997 hasRelatedWork W1968083340 @default.
• W2000504997 hasRelatedWork W2005057159 @default.
• W2000504997 hasRelatedWork W2025626092 @default.
• W2000504997 hasRelatedWork W2040478366 @default.
• W2000504997 hasRelatedWork W2063689836 @default.
• W2000504997 hasRelatedWork W2064585124 @default.
• W2000504997 hasRelatedWork W2087807076 @default.
• W2000504997 hasRelatedWork W2120419858 @default.
• W2000504997 hasRelatedWork W2405919697 @default.
• W2000504997 hasRelatedWork W2478414568 @default.
• W2000504997 hasRelatedWork W2513494236 @default.
• W2000504997 hasRelatedWork W2520857583 @default.
• W2000504997 hasRelatedWork W2553426767 @default.
• W2000504997 hasRelatedWork W77378452 @default.
• W2000504997 hasRelatedWork W2340018678 @default.
• W2000504997 isParatext "false" @default.
• W2000504997 isRetracted "false" @default.
• W2000504997 magId "2000504997" @default.
• W2000504997 workType "article" @default.