A-68930

A-68930
Nazivi
	IUPAC naziv (1R,3S)-1-(Aminometil)-3-fenil-3,4-dihidro-1H-izohromen-5,6-diol
Identifikacija
CAS broj	130465-45-1 ; 130465-39-3 (HCl) ;
3D model (Jmol)	interaktivna slika;
ChemSpider	109076 ;
MeSH	A+68930
PubChem C ID	122324;
	SMILES Oc1c(O)ccc2c1C[C@H](O[C@H]2CN)c3ccccc3; ; ; ; ; ;
Svojstva
Hemijska formula	C16H17NO3
Molarna masa	271,32 g·mol−1
log P	1,175
Kiselost (pKa)	9,491
Baznost (pKb)	4,506
	Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje materijala (na 25 °C [77 °F], 100 kPa).
	verifikuj (šta je ?)
	Reference infokutije

A-68930 je sintetičko jedinjenje koje deluje kao selektivni parcijalni agonist D₁.^[3]^[4] On je oralno aktivan i ima antidepresivno i anoreksično dejstvo na životinje, proizvodi budnost i tahikardiju,^[5]^[6]^[7]^[8] ali bez stimulansnih efekata, umesto toga uzrokuje sedaciju.^[9]^[10] 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.^[11]

Reference[uredi | uredi izvor]

^ 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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003. уреди
^ 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.
^ DeNinno MP, Schoenleber R, Asin KE, MacKenzie R, Kebabian JW (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. PMID 1977907. doi:10.1021/jm00173a005.
^ DeNinno MP, Schoenleber R, MacKenzie R, Britton DR, Asin KE, Briggs C, Trugman JM, Ackerman M, Artman L, Bednarz L (1991). „A68930: a potent agonist selective for the dopamine D1 receptor”. European Journal of Pharmacology. 199 (2): 209—19. PMID 1683288. doi:10.1016/0014-2999(91)90459-4.
^ Trampus M, Ferri N, Adami M, Ongini E (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. PMID 8100197. doi:10.1016/0014-2999(93)90823-Z.
^ Christie MI, Smith GW (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 (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 (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. PMID 7813561. doi:10.1016/0014-2999(94)90033-7.
^ Salmi P, Ahlenius S (2000). „Sedative effects of the dopamine D1 receptor agonist A 68930 on rat open-field behavior”. Neuroreport. 11 (6): 1269—72. PMID 10817605. doi:10.1097/00001756-200004270-00025.
^ 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. PMID 14960337. doi:10.1016/j.neuroscience.2003.11.016.
^ Nergårdh R, Oerther S, Fredholm BB (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. PMID 16318870. doi:10.1016/j.pbb.2005.09.017.

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[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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003. уреди

[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.

[pmid1977907-3] DeNinno MP, Schoenleber R, Asin KE, MacKenzie R, Kebabian JW (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. PMID 1977907. doi:10.1021/jm00173a005.

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

[pmid8100197-5] Trampus M, Ferri N, Adami M, Ongini E (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. PMID 8100197. doi:10.1016/0014-2999(93)90823-Z.

[pmid7906731-6] Christie MI, Smith GW (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.

[pmid11224270-7] AI-Naser HA, Cooper SJ (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.

[pmid7813561-8] D'Aquila PS, Collu M, Pani L, Gessa GL, Serra G (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. PMID 7813561. doi:10.1016/0014-2999(94)90033-7.

[pmid10817605-9] Salmi P, Ahlenius S (2000). „Sedative effects of the dopamine D1 receptor agonist A 68930 on rat open-field behavior”. Neuroreport. 11 (6): 1269—72. PMID 10817605. doi:10.1097/00001756-200004270-00025.

[pmid14960337-10] 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. PMID 14960337. doi:10.1016/j.neuroscience.2003.11.016.

[pmid16318870-11] Nergårdh R, Oerther S, Fredholm BB (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. PMID 16318870. doi:10.1016/j.pbb.2005.09.017.

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