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1992 1
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Page 1
The Discovery of Novel Selective D1 Dopaminergic Agonists: A-68930, A-77636, A-86929, and ABT-413.
Martin YC. Martin YC. Int J Med Chem. 2011;2011:424535. doi: 10.1155/2011/424535. Epub 2011 Mar 24. Int J Med Chem. 2011. PMID: 25954518 Free PMC article. Review.
The novel selective D1 dopaminergic full agonists A-68930, A-77636 were discovered by the synthesis of molecules to probe the bioactive conformation of the partial agonist SKF-38393, by the use of this information to add D1 affinity and selectivity to a screening hi …
The novel selective D1 dopaminergic full agonists A-68930, A-77636 were discovered by the synthesis of molecules to probe the …
A-77636: a potent and selective dopamine D1 receptor agonist with antiparkinsonian activity in marmosets.
Kebabian JW, Britton DR, DeNinno MP, Perner R, Smith L, Jenner P, Schoenleber R, Williams M. Kebabian JW, et al. Eur J Pharmacol. 1992 Dec 15;229(2-3):203-9. doi: 10.1016/0014-2999(92)90556-j. Eur J Pharmacol. 1992. PMID: 1362704
A-77636, ((1R,3S) 3-(1'-adamantyl)-1-aminomethyl-3,4-dihydro-5,6-dihydroxy-1H-2-benz opyran hydrochloride), is a selective dopamine D1 receptor agonist. In a battery of receptor binding assays, A-77636 shows the highest affinity (pKi = 7.40 +/- 0.09; K
A-77636, ((1R,3S) 3-(1'-adamantyl)-1-aminomethyl-3,4-dihydro-5,6-dihydroxy-1H-2-benz opyran hydrochloride), is a selective dop
Actions of the D1 agonists A-77636 and A-86929 on locomotion and dyskinesia in MPTP-treated L-dopa-primed common marmosets.
Pearce RK, Jackson M, Britton DR, Shiosaki K, Jenner P, Marsden CD. Pearce RK, et al. Psychopharmacology (Berl). 1999 Feb;142(1):51-60. doi: 10.1007/s002130050861. Psychopharmacology (Berl). 1999. PMID: 10102782
Several months later, L-dopa 12.5 mg/kg plus carbidopa 12.5 mg/kg was given orally twice daily for 7 days, followed by A-77636 1 micromol/kg for 10 days, and then both A-77636 and L-dopa plus carbidopa were given concurrently for 3 further days. ...Aft …
Several months later, L-dopa 12.5 mg/kg plus carbidopa 12.5 mg/kg was given orally twice daily for 7 days, followed by A-77636
Endogenous dopaminergic tone and dopamine agonist action.
Treseder SA, Smith LA, Jenner P. Treseder SA, et al. Mov Disord. 2000 Sep;15(5):804-12. doi: 10.1002/1531-8257(200009)15:5<804::aid-mds1007>3.0.co;2-2. Mov Disord. 2000. PMID: 11009183
Administration of quinpirole with A-77636 produced a reversal of motor deficits that was more resistant to AMPT pretreatment than was the effect produced by quinpirole or A-77636 alone. ...The reversal of motor deficits produced by the mixed D1/D2 agon …
Administration of quinpirole with A-77636 produced a reversal of motor deficits that was more resistant to AMPT pretreatment t …
The anorectic effect of the selective dopamine D1-receptor agonist A-77636 determined by meal pattern analysis in free-feeding rats.
Cooper SJ, Al-Naser HA, Clifton PG. Cooper SJ, et al. Eur J Pharmacol. 2006 Feb 27;532(3):253-7. doi: 10.1016/j.ejphar.2005.11.046. Epub 2006 Feb 14. Eur J Pharmacol. 2006. PMID: 16478622
In the present study, our aim was to investigate the effects of the dopamine D1-receptor agonist, A-77636 (0.1-1.0 mg/kg, s.c.), administered just prior to the start of the night period, on the free-feeding and drinking patterns of rats maintained on a standard ad l …
In the present study, our aim was to investigate the effects of the dopamine D1-receptor agonist, A-77636 (0.1-1.0 mg/kg, s.c. …
Nonstriatal dopamine D1 receptors regulate striatal acetylcholine release in vivo.
Acquas E, Wilson C, Fibiger HC. Acquas E, et al. J Pharmacol Exp Ther. 1997 Apr;281(1):360-8. J Pharmacol Exp Ther. 1997. PMID: 9103518
Local application of A-77636 (10 and 100 microM) by reverse dialysis was without effect on either striatal ACh or DA release. Systemic administration of the D1 DA receptor antagonist SCH 23390 (0.74 micromol/kg) or SCH 39166 (1.42 micromol/kg) blocked the stimulatio …
Local application of A-77636 (10 and 100 microM) by reverse dialysis was without effect on either striatal ACh or DA release. …
Persistent activation of the dopamine D1 receptor contributes to prolonged receptor desensitization: studies with A-77636.
Lin CW, Bianchi BR, Miller TR, Stashko MA, Wang SS, Curzon P, Bednarz L, Asin KE, Britton DR. Lin CW, et al. J Pharmacol Exp Ther. 1996 Mar;276(3):1022-9. J Pharmacol Exp Ther. 1996. PMID: 8786531
J. Pharmacol. 229: 203, 1992). However, A-77636 is of limited potential for PD therapy because it induces rapid tolerance in vivo. ...The residual cAMP activity declined with pretreatment time, and after 4-hr pretreatment, little residual cAMP production was observe …
J. Pharmacol. 229: 203, 1992). However, A-77636 is of limited potential for PD therapy because it induces rapid tolerance in v …
Comparison of interactions of D1-like agonists, SKF 81297, SKF 82958 and A-77636, with cocaine: locomotor activity and drug discrimination studies in rodents.
Chausmer AL, Katz JL. Chausmer AL, et al. Psychopharmacology (Berl). 2002 Jan;159(2):145-53. doi: 10.1007/s002130100896. Epub 2001 Sep 22. Psychopharmacology (Berl). 2002. PMID: 11862342
OBJECTIVES: The interactions of cocaine and A-77636 were compared to those obtained with the better investigated benzazepine D1-like dopamine agonists, SKF 82958 and SKF 81297. ...METHODS: Drug-naive Swiss-Webster mice were pretreated with SKF 81297, SKF 82958 or …
OBJECTIVES: The interactions of cocaine and A-77636 were compared to those obtained with the better investigated benzazepine D …
Effects of YM 435 and A 77636 on dopamine D-1 receptors in bovine retina in vitro.
Ofori S, De Raad S, Bugnon O, Schorderet M. Ofori S, et al. Gen Pharmacol. 1995 Jan;26(1):51-7. doi: 10.1016/0306-3623(94)00157-i. Gen Pharmacol. 1995. PMID: 7713366
Homogenates of bovine retinas were used to study the capacities of two new dopamine (DA) receptor agonists, e.g. YM 435 and A 77636, to interact with D1 receptors. 2. Adenylate cyclase experiments. YM 435 and A 77636 enhanced cAMP accumulation, with EC …
Homogenates of bovine retinas were used to study the capacities of two new dopamine (DA) receptor agonists, e.g. YM 435 and A 7763
The actions of a D-1 agonist in MPTP treated primates show dependence on both D-1 and D-2 receptor function and tolerance on repeated administration.
Smith LA, Jackson MJ, Al-Barghouthy G, Jenner P. Smith LA, et al. J Neural Transm (Vienna). 2002 Feb;109(2):123-40. doi: 10.1007/s007020200009. J Neural Transm (Vienna). 2002. PMID: 12075853
The potent and long acting D-1 receptor agonist, A-77636 reverses motor deficits in MPTP treated common marmosets following subcutaneous or oral administration. We now explore the effects of acute versus repeated administration of A-77636 and the relat …
The potent and long acting D-1 receptor agonist, A-77636 reverses motor deficits in MPTP treated common marmosets following su …
51 results