T A Pugsley
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Explore the profile of T A Pugsley including associated specialties, affiliations and a list of published articles.
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88
Citations
879
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Recent Articles
1.
Akunne H, Zoski K, Whetzel S, Cordon J, Brandon R, Roman F, et al.
Neuropharmacology
. 2001 Jul;
41(1):138-49.
PMID: 11445194
Igmesine is a selective sigma (sigma(1)) ligand that was reported to exert antidepressant action through an unknown mechanism of action. A number of neurochemical measures were taken in this study...
2.
Dooley D, Donovan C, Pugsley T
J Pharmacol Exp Ther
. 2000 Nov;
295(3):1086-93.
PMID: 11082444
Gabapentin (GBP; Neurontin) has proven efficacy in several neurological and psychiatric disorders yet its mechanism of action remains elusive. This drug, and the related compounds pregabalin [PGB; CI-1008, S-(+)-3-isobutylgaba] and...
3.
van Vliet L, Rodenhuis N, Wikstrom H, Pugsley T, Serpa K, Meltzer L, et al.
J Med Chem
. 2000 Sep;
43(19):3549-57.
PMID: 11000009
The 2-aminothiazole moiety has proven its value in medicinal chemistry as a stable and lipophilic bioisosteric replacement of a phenol group. This approach has provided dopamine (DA) agonists with good...
4.
van Vliet L, Rodenhuis N, Dijkstra D, Wikstrom H, Pugsley T, Serpa K, et al.
J Med Chem
. 2000 Aug;
43(15):2871-82.
PMID: 10956195
Benzopyranoxazine (+)-7 (PD 128907) is the most dopamine (DA) D3 receptor-selective agonist presently known. The only structural feature which distinguishes 7 from the analogous nonselective naphthoxazines is an oxygen atom...
5.
Corbin A, Meltzer L, NINTEMAN F, WILEY J, Christoffersen C, Wustrow D, et al.
Neuropharmacology
. 2000 Apr;
39(7):1211-21.
PMID: 10760363
PD 158771 has been described in receptor binding and biochemical tests as a partial agonist at dopamine (DA) D2 and D3 receptors as well as an agonist at serotonin (5-HT)(1A)...
6.
Akunne H, Zoski K, Davis M, Cooke L, Meltzer L, Whetzel S, et al.
Neuropharmacology
. 2000 Apr;
39(7):1197-210.
PMID: 10760362
The neurochemical effects of a novel dopamine (DA) D(2)-like and serotonin (5-HT) 5-HT(1A) agonist, PD 158771, are described. PD 158771 exhibited affinities for human D(2L), D(3) and D(4.2) receptors expressed...
7.
Belliotti T, Wustrow D, Brink W, Zoski K, Shih Y, Whetzel S, et al.
J Med Chem
. 1999 Dec;
42(25):5181-7.
PMID: 10602703
As part of a program to develop dopamine D4 antagonists for the treatment of schizophrenia, we discovered a series of 6- and 7-(phenylpiperazinyl)- and -(phenylpiperidinyl)methylbenzoxazinones through mass screening of our...
8.
Kesten S, Heffner T, Johnson S, Pugsley T, Wright J, Wise L
J Med Chem
. 1999 Sep;
42(18):3718-25.
PMID: 10479303
The discovery of a series of chromen-2-ones with selective affinity for the dopamine (DA) D4 receptor is described. Target compounds were tested for binding to cloned human DA D2L, D3,...
9.
Wustrow D, Capiris T, Rubin R, Knobelsdorf J, Akunne H, Davis M, et al.
Bioorg Med Chem Lett
. 1999 Jan;
8(16):2067-70.
PMID: 9873487
A series of 3-phenylpyrazolo[1,5-a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The 3-dimensional structure of one of the most potent analogs in this series, 10d,...
10.
Belliotti T, Brink W, Kesten S, Rubin J, Wustrow D, Zoski K, et al.
Bioorg Med Chem Lett
. 1999 Jan;
8(12):1499-502.
PMID: 9873377
PD 108635 (1) was identified as a potent dopamine D4 ligand and we wanted to replace the benzylic alcohol with a metabolically more stable moiety. Investigations led to the discovery...