A-68930

A-68930
	(1R,3S)-1-(Aminometil)-3-fenil-3,4-dihidro-1H-izohromen-5,6-diol
Identifikacija
CAS registarski broj	130465-45-1 , 130465-39-3 (HCl)
PubChem	122324
ChemSpider	109076
MeSH	A+68930
ChEMBL	CHEMBL315468
Jmol-3D slike	Slika 1
SMILES
	Oc1c(O)ccc2c1C[C@H](O[C@H]2CN)c3ccccc3
InChI
	InChI=InChI=1S/C16H17NO3/c17-9-15-11-6-7-13(18)16(19)12(11)8-14(20-15)10-4-2-1-3-5-10/h1-7,14-15,18-19H,8-9,17H2/t14-,15-/m0/s1 ; Kod: SUHGRZPINGKYNV-GJZGRUSLSA-N
Svojstva
Molekulska formula	C16H17NO3
Molarna masa	271.31 g mol−1
log P	1,175
pKa	9,491
Baznost (pKb)	4,506
	(šta je ovo?) (verifikuj) ; Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje (25 °C, 100 kPa) materijala
	Infobox references

A-68930 je sintetičko jedinjenje koje deluje kao selektivni parcijalni agonist D₁.^[5]^[6] On je oralno aktivan i ima antidepresivno i anoreksično dejstvo na životinje, proizvodi budnost i tahikardiju,^[7]^[8]^[9]^[10] ali bez stimulansnih efekata, umesto toga uzrokuje sedaciju.^[11]^[12] Moguće je da je razlika u dejstvu između A-68930 i drugih D₁ agonista kao što je SKF-82958 posledica različitih efekata na srodni D₅ receptor.^[13]

Reference uredi

↑ 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
↑ DeNinno MP, Schoenleber R, Asin KE, MacKenzie R, Kebabian JW (November 1990). „(1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist”. Journal of Medicinal Chemistry 33 (11): 2948–50. DOI:10.1021/jm00173a005. PMID 1977907.
↑ DeNinno MP, Schoenleber R, MacKenzie R, Britton DR, Asin KE, Briggs C, Trugman JM, Ackerman M, Artman L, Bednarz L (June 1991). „A68930: a potent agonist selective for the dopamine D1 receptor”. European Journal of Pharmacology 199 (2): 209–19. DOI:10.1016/0014-2999(91)90459-4. PMID 1683288.
↑ Trampus M, Ferri N, Adami M, Ongini E (April 1993). „The dopamine D1 receptor agonists, A68930 and SKF 38393, induce arousal and suppress REM sleep in the rat”. European Journal of Pharmacology 235 (1): 83–7. DOI:10.1016/0014-2999(93)90823-Z. PMID 8100197.
↑ Christie MI, Smith GW (February 1994). „Cardiovascular and renal hemodynamic effects of A-68930 in the conscious dog: a comparison with fenoldopam”. The Journal of Pharmacology and Experimental Therapeutics 268 (2): 565–70. PMID 7906731.
↑ AI-Naser HA, Cooper SJ (April 1994). „A-68930, a novel, potent dopamine D1 receptor agonist: a microstructural analysis of its effects on feeding and other behaviour in the rat”. Behavioural Pharmacology 5 (2): 210–218. PMID 11224270.
↑ D'Aquila PS, Collu M, Pani L, Gessa GL, Serra G (September 1994). „Antidepressant-like effect of selective dopamine D1 receptor agonists in the behavioural despair animal model of depression”. European Journal of Pharmacology 262 (1–2): 107–11. DOI:10.1016/0014-2999(94)90033-7. PMID 7813561.
↑ Salmi P, Ahlenius S (April 2000). „Sedative effects of the dopamine D1 receptor agonist A 68930 on rat open-field behavior”. Neuroreport 11 (6): 1269–72. DOI:10.1097/00001756-200004270-00025. PMID 10817605.
↑ Isacson R, Kull B, Wahlestedt C, Salmi P (2004). „A 68930 and dihydrexidine inhibit locomotor activity and d-amphetamine-induced hyperactivity in rats: a role of inhibitory dopamine D(1/5) receptors in the prefrontal cortex?”. Neuroscience 124 (1): 33–42. DOI:10.1016/j.neuroscience.2003.11.016. PMID 14960337.
↑ Nergårdh R, Oerther S, Fredholm BB (November 2005). „Differences between A 68930 and SKF 82958 could suggest synergistic roles of D1 and D5 receptors”. Pharmacology, Biochemistry, and Behavior 82 (3): 495–505. DOI:10.1016/j.pbb.2005.09.017. PMID 16318870.

[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

[pmid1977907-5] DeNinno MP, Schoenleber R, Asin KE, MacKenzie R, Kebabian JW (November 1990). „(1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist”. Journal of Medicinal Chemistry 33 (11): 2948–50. DOI:10.1021/jm00173a005. PMID 1977907.

[pmid1683288-6] DeNinno MP, Schoenleber R, MacKenzie R, Britton DR, Asin KE, Briggs C, Trugman JM, Ackerman M, Artman L, Bednarz L (June 1991). „A68930: a potent agonist selective for the dopamine D1 receptor”. European Journal of Pharmacology 199 (2): 209–19. DOI:10.1016/0014-2999(91)90459-4. PMID 1683288.

[pmid8100197-7] Trampus M, Ferri N, Adami M, Ongini E (April 1993). „The dopamine D1 receptor agonists, A68930 and SKF 38393, induce arousal and suppress REM sleep in the rat”. European Journal of Pharmacology 235 (1): 83–7. DOI:10.1016/0014-2999(93)90823-Z. PMID 8100197.

[pmid7906731-8] Christie MI, Smith GW (February 1994). „Cardiovascular and renal hemodynamic effects of A-68930 in the conscious dog: a comparison with fenoldopam”. The Journal of Pharmacology and Experimental Therapeutics 268 (2): 565–70. PMID 7906731.

[pmid11224270-9] AI-Naser HA, Cooper SJ (April 1994). „A-68930, a novel, potent dopamine D1 receptor agonist: a microstructural analysis of its effects on feeding and other behaviour in the rat”. Behavioural Pharmacology 5 (2): 210–218. PMID 11224270.

[pmid7813561-10] D'Aquila PS, Collu M, Pani L, Gessa GL, Serra G (September 1994). „Antidepressant-like effect of selective dopamine D1 receptor agonists in the behavioural despair animal model of depression”. European Journal of Pharmacology 262 (1–2): 107–11. DOI:10.1016/0014-2999(94)90033-7. PMID 7813561.

[pmid10817605-11] Salmi P, Ahlenius S (April 2000). „Sedative effects of the dopamine D1 receptor agonist A 68930 on rat open-field behavior”. Neuroreport 11 (6): 1269–72. DOI:10.1097/00001756-200004270-00025. PMID 10817605.

[pmid14960337-12] Isacson R, Kull B, Wahlestedt C, Salmi P (2004). „A 68930 and dihydrexidine inhibit locomotor activity and d-amphetamine-induced hyperactivity in rats: a role of inhibitory dopamine D(1/5) receptors in the prefrontal cortex?”. Neuroscience 124 (1): 33–42. DOI:10.1016/j.neuroscience.2003.11.016. PMID 14960337.

[pmid16318870-13] Nergårdh R, Oerther S, Fredholm BB (November 2005). „Differences between A 68930 and SKF 82958 could suggest synergistic roles of D1 and D5 receptors”. Pharmacology, Biochemistry, and Behavior 82 (3): 495–505. DOI:10.1016/j.pbb.2005.09.017. PMID 16318870.

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