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Review

Lead generation and lead optimisation approaches in the discovery of selective, non-peptide ORL-1 receptor agonists and antagonists

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Pages 525-546 | Published online: 25 Feb 2005

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  • •Detailed SAR study disclosing very high affinity ORL-1 receptor agonists.
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  • ••Disclosure of Ro 64–6198, a selective ORL-1 receptor agonistwith in vivo anxiolytic activity.
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  • ••Disclosure of J-113397, the first non-peptide, selectiveORL-1 antagonist.
  • OZAKI S, KAWAMOTO H, ITOH Y, MIYAJI M, IWASAWA Y, OHTA H: A potent and highly selective nonpeptidyl nociceptin/orphanin FQ receptor (ORLI) antagonist: J-113397. Eur.J. Pharmacol (2000) 387:R17–R18.
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  • •Extensive pharmacological characterisation of J-113397.
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  • •Disclosure of JTC-801, a non-peptide ORL-1 antagonist with in vivo activity.

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