J E Lachowicz
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Explore the profile of J E Lachowicz including associated specialties, affiliations and a list of published articles.
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21
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646
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Recent Articles
1.
Sasikumar T, Burnett D, Zhang H, Smith-Torhan A, Fawzi A, Lachowicz J
Bioorg Med Chem Lett
. 2006 Jul;
16(17):4543-7.
PMID: 16809034
Acylated and aroylated hydrazinoclozapines are highly potent dopamine D(1) antagonists that show remarkable selectivity over other dopamine receptors. The most potent compound in this series is the 2,6-dimethoxybenzhydrazide 33 with...
2.
Randolph G, Simon J, Arreaza M, Qiu P, Lachowicz J, Duffy R
Pharmacogenomics J
. 2004 Sep;
4(6):394-402.
PMID: 15452552
Neurokinin receptors in the central nervous system are involved in the neural circuitry of anxiety, depression and emesis. This has led to the development of nonpeptidic NK1 receptor antagonists as...
3.
Duffy R, Hedrick J, Randolph G, Morgan C, Cohen-Williams M, Vassileva G, et al.
Neuropharmacology
. 2003 Jul;
45(2):242-50.
PMID: 12842130
Hemokinin-1 (HK-1) is a recently described mouse tachykinin peptide whose biological functions are not fully understood. To date, a unique receptor for HK-1 has not been identified. Recent studies suggest...
4.
Boyle C, Chackalamannil S, Clader J, Greenlee W, Josien H, Kaminski J, et al.
Bioorg Med Chem Lett
. 2001 Aug;
11(17):2311-4.
PMID: 11527721
The potential toxicological liabilities of the M(2) muscarinic antagonist 1 were addressed by replacing the methylenedioxyphenyl moiety with a p-methoxyphenyl group, resulting in M(2) selective compounds such as 3. Several...
5.
Foster C, Prosser D, Agans J, Zhai Y, Smith M, Lachowicz J, et al.
J Clin Invest
. 2001 Jun;
107(12):1591-8.
PMID: 11413167
ADP plays a critical role in modulating thrombosis and hemostasis. ADP initiates platelet aggregation by simultaneous activation of two G protein-coupled receptors, P2Y1 and P2Y12. Activation of P2Y1 activates phospholipase...
6.
Lachowicz J, Duffy R, Ruperto V, Kozlowski J, Zhou G, Clader J, et al.
Life Sci
. 2001 Jun;
68(22-23):2585-92.
PMID: 11392630
Current treatment of Alzheimer's Disease (AD) requires acetylcholinesterase inhibition to increase acetylcholine (ACh) concentrations in the synaptic cleft. Another mechanism by which ACh levels can be increased is blockade of...
7.
Wang Y, Chackalamannil S, Chang W, Greenlee W, Ruperto V, Duffy R, et al.
Bioorg Med Chem Lett
. 2001 Apr;
11(7):891-4.
PMID: 11294385
Novel, selective M2 muscarinic antagonists, which replace the metabolically labile styrenyl moiety of the prototypical M2 antagonist 1 with an ether linkage, were synthesized. A detailed SAR study in this...
8.
Boyle C, Chackalamannil S, Chen L, Dugar S, Pushpavanam P, Billard W, et al.
Bioorg Med Chem Lett
. 2001 Jan;
10(24):2727-30.
PMID: 11133078
Benzylidene ketal derivatives were investigated as selective M2 receptor antagonists for the treatment of Alzheimer's disease. Compound 10 was discovered to have subnanomolar M2 receptor affinity and 100-fold selectivity against...
9.
Kozlowski J, Lowe D, Guzik H, Zhou G, Ruperto V, Duffy R, et al.
Bioorg Med Chem Lett
. 2000 Oct;
10(20):2255-7.
PMID: 11055332
Structure activity studies on [4-(phenylsulfonyl)phenyl]methylpiperazine led to the discovery of 4-cyclohexyl-alpha-[4-[[4-methoxyphenyl(S)-sufinyl]phenyl]-1-pi perazineacetonitrile, 1, an M2 selective muscarinic antagonist. Affinity at the cloned human M2 receptor was 2.7 nM; the M1/M2...
10.
Wang Y, Chackalamannil S, Hu Z, Clader J, Greenlee W, Billard W, et al.
Bioorg Med Chem Lett
. 2000 Oct;
10(20):2247-50.
PMID: 11055330
Identification of a number of highly potent M2 receptor antagonists with >100-fold selectivity against the M1 and M3 receptor subtypes is described. In the rat microdialysis assay, this series of...