A-412,997

A-412,997
(IUPAC) ime
	N-(3-metilfenil)-2-(4-piridin-2-ilpiperidin-1-il)acetamid
Klinički podaci
Identifikatori
ATC kod	nije dodeljen
PubChem	10425450
ChemSpider	8600878
ChEMBL	CHEMBL375596
Hemijski podaci
Formula	C19H23N3O
Mol. masa	309,405 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C19H23N3O/c1-15-5-4-6-17(13-15)21-19(23)14-22-11-8-16(9-12-22)18-7-2-3-10-20-18/h2-7,10,13,16H,8-9,11-12,14H2,1H3,(H,21,23) ; Key: JFCDMGGMCUKHST-UHFFFAOYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

A-412,997 je lek koji deluje kao dopaminski agonist i koji se koristi u naučnim istraživanjima. On je bio prvi lek sa visokom selektivnošću za D₄ podtip. Njegova selektivnost je znatno veća od starijih D₄ jedinjenja poput PD-168,077 i CP-226,269.^[5] U životinjskim testovima je pokazano da on poboljšava kognitivne sposobnosti pacova u sličnoj meri kao i metilfenidat, ali bez neželjenih efekata.^[6]^[7] Za razliku od drugih dopaminskih agonista, selektivni D₄ agonisti ne proizvode sporedne efekte kao što je sedacija i mučnina, tako da imaju prednost u odnosu na starije dopaminske agoniste.^[8]

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ Moreland RB, Patel M, Hsieh GC, Wetter JM, Marsh K, Brioni JD (2005). „A-412997 is a selective dopamine D4 receptor agonist in rats”. Pharmacology, biochemistry, and behavior 82 (1): 140–7. DOI:10.1016/j.pbb.2005.08.001. PMID 16153699.
↑ Browman KE, Curzon P, Pan JB, Molesky AL, Komater VA, Decker MW, Brioni JD, Moreland RB, Fox GB (2005). „A-412997, a selective dopamine D4 agonist, improves cognitive performance in rats”. Pharmacology, biochemistry, and behavior 82 (1): 148–55. DOI:10.1016/j.pbb.2005.08.002. PMID 16154186.
↑ Woolley ML, Waters KA, Reavill C, Bull S, Lacroix LP, Martyn AJ, Hutcheson DM, Valerio E, Bate S, Dawson LA, Jones DN (December 2008). „Selective dopamine D4 receptor agonist (A-412997) improves cognitive performance and stimulates motor activity without influencing reward-related behaviour in rat”. Behavioural Pharmacology 19 (8): 765–76. DOI:10.1097/FBP.0b013e32831c3b06. PMID 19020411.
↑ Osinski MA, Uchic ME, Seifert T, Shaughnessy TK, Miller LN, Nakane M, Cox BF, Brioni JD, Moreland RB (2005). „Dopamine D2, but not D4, receptor agonists are emetogenic in ferrets”. Pharmacology, biochemistry, and behavior 81 (1): 211–9. DOI:10.1016/j.pbb.2005.03.012. PMID 15894081.

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[4] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[5] Moreland RB, Patel M, Hsieh GC, Wetter JM, Marsh K, Brioni JD (2005). „A-412997 is a selective dopamine D4 receptor agonist in rats”. Pharmacology, biochemistry, and behavior 82 (1): 140–7. DOI:10.1016/j.pbb.2005.08.001. PMID 16153699.

[6] Browman KE, Curzon P, Pan JB, Molesky AL, Komater VA, Decker MW, Brioni JD, Moreland RB, Fox GB (2005). „A-412997, a selective dopamine D4 agonist, improves cognitive performance in rats”. Pharmacology, biochemistry, and behavior 82 (1): 148–55. DOI:10.1016/j.pbb.2005.08.002. PMID 16154186.

[pmid19020411-7] Woolley ML, Waters KA, Reavill C, Bull S, Lacroix LP, Martyn AJ, Hutcheson DM, Valerio E, Bate S, Dawson LA, Jones DN (December 2008). „Selective dopamine D4 receptor agonist (A-412997) improves cognitive performance and stimulates motor activity without influencing reward-related behaviour in rat”. Behavioural Pharmacology 19 (8): 765–76. DOI:10.1097/FBP.0b013e32831c3b06. PMID 19020411.

[8] Osinski MA, Uchic ME, Seifert T, Shaughnessy TK, Miller LN, Nakane M, Cox BF, Brioni JD, Moreland RB (2005). „Dopamine D2, but not D4, receptor agonists are emetogenic in ferrets”. Pharmacology, biochemistry, and behavior 81 (1): 211–9. DOI:10.1016/j.pbb.2005.03.012. PMID 15894081.

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