P Jeffrey Conn
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Explore the profile of P Jeffrey Conn including associated specialties, affiliations and a list of published articles.
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403
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Recent Articles
1.
Giona F, Beretta S, Zippo A, Stefanoni A, Tomasoni Z, Vicidomini C, et al.
Mol Psychiatry
. 2025 Mar;
PMID: 40089604
Mutations or deletions in the SHANK3 gene have been identified in up to 1% of autism spectrum disorder cases and are considered the primary cause of neuropsychiatric symptoms in Phelan...
2.
Reed C, Kalbfleisch J, Turkett J, Trombley T, Spearing P, Haymer D, et al.
ACS Chem Neurosci
. 2025 Feb;
16(4):745-752.
PMID: 39907715
Herein, we report the further chemical optimization of the metabotropic glutamate receptor subtype 1 (mGlu) positive allosteric modulator (PAM) VU6024578/BI02982816 and the discovery of VU6033685/BI1752. PAM VU6033685/BI1752 was developed through...
3.
Childress E, Capstick R, Crocker K, Ledyard M, Bender A, Maurer M, et al.
ACS Med Chem Lett
. 2024 Dec;
15(12):2210-2219.
PMID: 39691522
This Letter details our efforts to develop novel, non-acetylene-containing metabotropic glutamate receptor subtype 5 (mGlu) negative allosteric modulators (NAMs) with improved pharmacological properties. This endeavor involved replacing the ether-linked pyrimidine...
4.
Reed C, Kalbfleisch J, Turkett J, Trombley T, Nastase A, Spearing P, et al.
J Med Chem
. 2024 Dec;
67(24):22291-22312.
PMID: 39665415
Herein, we report progress toward a metabotropic glutamate receptor subtype 1 (mGlu) positive allosteric modulator (PAM) clinical candidate and the discovery of VU6024578/BI02982816. From a weak high-throughput screening hit (VU0538160,...
5.
Poslunsey M, Wood M, Han C, Stauffer S, Panarese J, Melancon B, et al.
ACS Chem Neurosci
. 2024 Dec;
16(1):95-107.
PMID: 39660766
Herein we detail the of VU0467319 (VU319), an M Positive Allosteric Modulator (PAM) clinical candidate that successfully completed a Phase I Single Ascending Dose (SAD) clinical trial. VU319 () is...
6.
Engers J, Baker L, Chang S, Luscombe V, Rodriguez A, Niswender C, et al.
ACS Chem Neurosci
. 2024 Sep;
PMID: 39316465
Herein, we report structure-activity relationship (SAR) studies to develop novel tricyclic M PAM scaffolds with improved pharmacological properties. This endeavor involved a "tie-back" strategy to replace a 5-amino-2,4-dimethylthieno[2,3-]pyrimidine-6-carboxamide core, which...
7.
Engers J, Bollinger K, Capstick R, Long M, Bender A, Dickerson J, et al.
ACS Chem Neurosci
. 2024 Aug;
15(18):3421-3433.
PMID: 39197083
Herein we report progress toward a backup clinical candidate to the M positive allosteric modulator (PAM) VU319/ACP-319. Scaffold-hopping from the pyrrolo[2,3-]pyridine-based M PAM VU6007477 to isomeric pyrrolo[3,2-]pyridine and thieno[3,2-]pyridine congeners...
8.
Capstick R, Bollinger S, Engers J, Long M, Chang S, Luscombe V, et al.
ACS Med Chem Lett
. 2024 Aug;
15(8):1358-1366.
PMID: 39140069
This Letter details our efforts to develop novel tricyclic muscarinic acetylcholine receptor subtype 4 (M) positive allosteric modulator (PAM) scaffolds with improved pharmacological properties. This endeavor involved a "tie-back" strategy...
9.
Li J, Orsi D, Engers J, Long M, Capstick R, Maurer M, et al.
J Med Chem
. 2024 Aug;
67(16):14394-14413.
PMID: 39105778
While the muscarinic acetylcholine receptor mAChR subtype 5 (M) has been studied over decades, recent findings suggest that more in-depth research is required to elucidate a thorough understanding of its...
10.
Balakrishnan A, Johansen L, Lindsley C, Conn P, Thomsen M
Prog Neuropsychopharmacol Biol Psychiatry
. 2024 Jul;
134:111079.
PMID: 38950842
Acute stimulation of M or M muscarinic cholinergic receptors reduces cocaine abuse-related effects in mice and rats. The combined activation of these receptor subtypes produces synergistic effects on some behavioural...