Severity: Warning
Message: file_get_contents(https://...@gmail.com&api_key=61f08fa0b96a73de8c900d749fcb997acc09): Failed to open stream: HTTP request failed! HTTP/1.1 429 Too Many Requests
Filename: helpers/my_audit_helper.php
Line Number: 143
Backtrace:
File: /var/www/html/application/helpers/my_audit_helper.php
Line: 143
Function: file_get_contents
File: /var/www/html/application/helpers/my_audit_helper.php
Line: 209
Function: simplexml_load_file_from_url
File: /var/www/html/application/helpers/my_audit_helper.php
Line: 3098
Function: getPubMedXML
File: /var/www/html/application/controllers/Detail.php
Line: 574
Function: pubMedSearch_Global
File: /var/www/html/application/controllers/Detail.php
Line: 488
Function: pubMedGetRelatedKeyword
File: /var/www/html/index.php
Line: 316
Function: require_once
Severity: Warning
Message: Attempt to read property "Count" on bool
Filename: helpers/my_audit_helper.php
Line Number: 3100
Backtrace:
File: /var/www/html/application/helpers/my_audit_helper.php
Line: 3100
Function: _error_handler
File: /var/www/html/application/controllers/Detail.php
Line: 574
Function: pubMedSearch_Global
File: /var/www/html/application/controllers/Detail.php
Line: 488
Function: pubMedGetRelatedKeyword
File: /var/www/html/index.php
Line: 316
Function: require_once
Orexin 1 receptor (OXR) is thought to be involved in various body functions, including arousal maintenance and emotional control, but the full details of its function remain unknown. OXR imaging with positron emission tomography (PET) would be useful in elucidating the orexin system including OXR, but no PET probes targeting OXR have been reported. We, therefore, designed and synthesized tetrahydroisoquinoline (THIQ) derivatives as novel PET probes targeting OXR, and evaluated their utility. In an in vitro competitive binding assay, THIQ-1 and THIQ-2 showed significantly higher binding to OXR (IC = 30 and 31 nM, respectively) than OXR (IC = 160 and 332 nM, respectively). These features were also observed in a cell binding assay using [F]THIQ-1 and [F]THIQ-2, demonstrating their OXR-specific binding property in vitro. In a biodistribution study using normal mice, the brain uptake of [F]THIQ-1 was higher than that of [F]THIQ-2, but further improvement is required for in vivo imaging with PET. Taken together, [F]THIQ-1 and [F]THIQ-2 have the potential to become useful imaging probes for PET targeting the OXR, but require additional structural changes to improve their brain uptake.
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Source |
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http://dx.doi.org/10.1016/j.bmcl.2019.04.044 | DOI Listing |
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