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Journal: Design and discovery of a high affinity, selective and β-arrestin biased 5-HT Receptor Agonist. (Pubmed Central) - Mar 29, 2022 Although 2a showed about 8 times less activity than 5-HT in the Gs pathway, it showed over 31 times higher activity than 5-HT in the β-arrestin pathway. This constitutes a significant β-arrestin pathway preference and shows 2a to be more potent and more efficacious than the recently published β-arrestin biased 3-(4-chlorophenyl)-1,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepine, the N-debenzylated analog of JNJ18038683 (Compound 7).
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Enrollment closed, Trial completion date: Testing the Ability of JNJ-18038683 to Improve Cognition and Reduce Depressive Symptoms in Stable Bipolar Patients (clinicaltrials.gov) - Jan 19, 2022 P2, N=60, Active, not recruiting, This constitutes a significant β-arrestin pathway preference and shows 2a to be more potent and more efficacious than the recently published β-arrestin biased 3-(4-chlorophenyl)-1,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepine, the N-debenzylated analog of JNJ18038683 (Compound 7). Recruiting --> Active, not recruiting | Trial completion date: Dec 2021 --> Dec 2022
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Trial completion date, Trial primary completion date: Imaging 5HT7 Antagonist Effects in Bipolar Disorder (clinicaltrials.gov) - Sep 8, 2021 P=N/A, N=68, Recruiting, Trial completion date: Oct 2019 --> Dec 2021 | Trial primary completion date: Jul 2019 --> Sep 2021 Trial completion date: Jul 2020 --> Jun 2022 | Trial primary completion date: May 2020 --> Jun 2022
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