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32 results on '"Jeffrey Conn, P."'

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1. Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds

2. Development of structurally distinct tricyclic M4 positive allosteric modulator (PAM) chemotypes - Part 2

3. Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M1

5. Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs

10. Discovery of 4-alkoxy-6-methylpicolinamide negative allosteric modulators of metabotropic glutamate receptor subtype 5

11. The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate

12. Corrigendum to “Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides” [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179–5184]

16. Discovery of ML326: The first sub-micromolar, selective M5 PAM

18. Discovery and SAR of a novel series of non-MPEP site mGlu5 PAMs based on an aryl glycine sulfonamide scaffold

19. Corrigendum to “Development of a scintillation proximity assay for analysis of Na+/Cl− -dependent neurotransmitter transporter activity” [Anal. Biochem. 321 (2003) 31–37]

20. Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor

21. Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012

22. Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM

24. Development of a more highly selective M1 antagonist from the continued optimization of the MLPCN Probe ML012

31. Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties

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