{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,24]],"date-time":"2026-09-24T18:19:02Z","timestamp":1790273942189,"version":"4.1.0"},"reference-count":37,"publisher":"Oxford University Press (OUP)","issue":"10","license":[{"start":{"date-parts":[[2004,10,1]],"date-time":"2004-10-01T00:00:00Z","timestamp":1096588800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/academic.oup.com\/journals\/pages\/open_access\/funder_policies\/chorus\/standard_publication_model"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2004,10,1]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>Twenty agonists and nine antagonists were evaluated for their ability to compete for [3H]-8-hydroxy-2-(di-n-propylamino)tetralin ([3H]-8-OH-DPAT) binding to the cloned human serotonin-1A (ch-5-HT1A) receptor expressed in Chinese hamster ovary cells and for their ability to alter adenylyl cyclase activity in the same cells. The most potent full agonists of high affinity included N,N-dipropyl-5-carboxamidotryptamine (pEC50 = 9.6 \u00b1 0.1), MDL 73005EF (pEC50 = 9.3 \u00b1 0.2), 5-methyl-urapidil (pEC50 = 9.2 \u00b1 0.1), 5-carboxamidotryptamine (pEC50 = 9.1 \u00b1 0.2), R(+)-8-OH-DPAT (pEC50 = 8.6 \u00b1 0.1) and BMY-7378 (pEC50 = 8.6 \u00b1 0.1). WB-4101 (pEC50 = 8.3 \u00b1 0.2; IA = 79%), clozapine (pEC50 = 8.1 \u00b1 0.3; IA = 29%), (buspirone (pEC50 = 7.6 \u00b1 0.2; IA = 79%), quipazine (pEC50&amp;lt;5; IA = 45%) and R-DOI (pEC50&amp;lt;5; IA = 31%) were weaker agonists with partial agonist properties. The most potent antagonists were WAY-100,635 (pKi = 10.2 \u00b1 0.1), methiothepin (pKi = 8.8 \u00b1 0.2), spiperone (pKi = 8.7 \u00b1 0.2) and NAN-190 (pKi = 8.5 \u00b1 0.2). The receptor affinities and functional potencies were well correlated (r = 0.88; P&amp;lt;0.0001). Our binding data correlated well with the pharmacology of endogenous 5-HT1A receptors in the rabbit iris-ciliary body (r = 0.91; P&amp;lt;0.001) and rat hippocampus (r = 0.93, P&amp;lt;0.0001). Our functional cAMP data correlated well with other cAMP accumulation data (r = 0.8, P&amp;lt;0.01 vs calf hippocampus) but less so with [35S]-GTP-yS binding to the ch-5-HT1A receptor as a functional activity read-out (r = 0.58, P&amp;lt;0.05). The present study provides a detailed pharmacological characterization of the ch-5-HT1A receptor using binding and functional assays.<\/jats:p>","DOI":"10.1211\/0022357044346","type":"journal-article","created":{"date-parts":[[2004,9,28]],"date-time":"2004-09-28T18:38:46Z","timestamp":1096396726000},"page":"1267-1274","source":"Crossref","is-referenced-by-count":20,"title":["Cloned human 5-HT1A receptor pharmacology determined using agonist binding and measurement of cAMP accumulation"],"prefix":"10.1093","volume":"56","author":[{"given":"Najam A","family":"Sharif","sequence":"first","affiliation":[{"name":"Molecular Pharmacology Unit, Pharmaceutical Products Research, Alcon Research, Ltd , Fort Worth, TX 76134-2099,","place":["USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Colene D","family":"Drace","sequence":"additional","affiliation":[{"name":"Molecular Pharmacology Unit, Pharmaceutical Products Research, Alcon Research, Ltd , Fort Worth, TX 76134-2099,","place":["USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gary W","family":"Williams","sequence":"additional","affiliation":[{"name":"Molecular Pharmacology Unit, Pharmaceutical Products Research, Alcon Research, Ltd , Fort Worth, TX 76134-2099,","place":["USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Julie Y","family":"Crider","sequence":"additional","affiliation":[{"name":"Molecular Pharmacology Unit, Pharmaceutical Products Research, Alcon Research, Ltd , Fort Worth, TX 76134-2099,","place":["USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"286","published-online":{"date-parts":[[2004,10,1]]},"reference":[{"key":"2024103109411528300_cit1","first-page":"508","article-title":"Functional characterization of the recombinant human 5-hydroxytryptamine7(a) receptor isoform coupled to adenylate cyclase stimulation","volume":"287","author":"Adham","year":"1998","journal-title":"J. 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