In silico study of naphtha [1, 2-d] thiazol-2-amine with adenosine A 2A receptor and its role in antagonism of haloperidol-induced motor impairments in mice.
Loss of dopaminergic nigrostriatal neurons in the substantia nigra leads to Parkinson's disease (PD). Adenosine A(2A) receptors (A(2A)Rs) have been anticipated as novel therapeutic target for PD. A(2A)Rs potentiate locomotor behavior and are predominantly expressed in striatum. Naphtha [1, 2-d] thiazol-2-amine (NATA), a tricyclic thiazole have been studied as new anti-Parkinsonian compound. AutoDock analysis and pharmacophore study of NATA with known A(2A)R antagonists explicit its efficacy as a possible adenosine receptor antagonist. In vivo pharmacology of NATA showed reduction of haloperidol (HAL)-induced motor impairments in Swiss albino male mice. Relatively elevated levels of dopamine in NATA pre-treated mice are suggestive of its possible role as neuromodulator in PD.
Luthra
Pratibha Mehta
PM
Medicinal Chemistry Division, Dr. B.R. Ambedkar Center for Biomedical Research, University of Delhi, North Campus, Mall Road, Delhi 110007, India. pmluthra@acbr.du.ac.in
Prakash
Amresh
A
Barodia
Sandeep Kumar
SK
Kumari
Rita
R
Mishra
Chandra Bhushan
CB
Kumar
J B Senthil
JB
D058917:Adenosine A2 Receptor Antagonists; D000818:Animals; D003342:Corpus Striatum / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism; D006220:Haloperidol; D006801:Humans; D008297:Male; D051379:Mice; D008958:Models, Molecular; D009043:Motor Activity / Q000187:drug effects*; D009069:Movement Disorders / Q000209:etiology / Q000503:physiopathology / Q000517:prevention & control*; D009281:Naphthalenes / Q000737:chemistry* / Q000494:pharmacology*; D043705:Receptor, Adenosine A2A / Q000737:chemistry; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology*; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology*
D058917:Adenosine A2 Receptor Antagonists; D009281:Naphthalenes; D043705:Receptor, Adenosine A2A; D013844:Thiazoles; D014230:Triazoles; C545482:naphtha(1,2-d)thiazol-2-amine; D006220:Haloperidol; D004298:Dopamine