Detail of "81633-77-4"

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Selective and stereospecific interactions of R-SK & F 38393 with [3H]piflutixol but not [3H]spiperone binding to striatal D1 and D2 dopamine receptors: comparisons with SCH 23390

Selective and stereospecific interactions of R-SK & F 38393 with [3H]piflutixol but not [3H]spiperone binding to striatal D1 and D2 dopamine receptors: comparisons with SCH 23390. O'Boyle, Kathy M.; Waddington, John L. (Dep. Clin. Pharmacol., R. 81633-77-4 and 50-53-3 are cas registry numbers. These chemicals are also mentioned in this article. Coll. Surg. Ireland, Dublin, Ire.). Eur. J. Pharmacol., 98(3-4), 433-6 (English) 1984. CODEN: EJPHAZ. ISSN: 0014-2999. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 2 Four benzazepine derivs., racemic SK & F 38393 [81633-77-4], its resolved R- [62751-59-1] and S-enantiomer [81702-43-4], and SCH 23390 [87134-87-0] were investigated for their interactions with striatal D1 and D2 dopamine receptors, as indexed by the binding of 3H-labeled piflutixol [54341-02-5] and 3H-labeled spiperone [749-02-0], resp. For the agonist SK & F 38393, its R-enantiomer was active in displacing [3H]piflutixol while its S-antipode was 100-fold less potent. In contrast, both enantiomers showed similar and negligible activity to displace [3H]spiperone. SCH 23390, an antagonist analog with an R-configuration, potently displaced [3H]piflutixol but not [3H]spiperone. R-SK & F 38393 and SCH 23390 may help clarify the structural requirements for, and functional consequences of, selective actions at the D1 dopamine receptor. .

Effects of chronic treatment with selective agonists on the subtypes of dopamine receptors

Effects of chronic treatment with selective agonists on the subtypes of dopamine receptors. Subramaniam, Swaminathan; Lucki, Irwin; McGonigle, Paul (Sch. Med., Univ. Pennsylvania, Philadelphia, PA 19104, USA). Brain Res., 571(2), 313-22 (English) 1992. CODEN: BRREAP. ISSN: 0006-8993. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 2 The effects of chronic administration of selective dopaminergic agonists on D1 and D2 receptor d., affinity, and function were measured in Sprague-Dawley rats. Animals received daily injections (i.p.) of the D1-selective agonist SKF-38393 (10 mg/kg), the D2-selective agonist quinpirole (1 mg/kg), SKF-38393 plus quinpirole, or saline for 14 days. Quant. autoradiog.Several substances with their cas registry numbers 81633-77-4 and 80373-22-4 may be metioned in this study. anal. revealed that the d. of D2 receptors was decreased following chronic treatment with quinpirole alone or in combination with SKF-38393 whereas SKF-38393 by itself had no effect on this receptor. In contrast, the d. of D1 receptors was increased following treatment with SKF-38393. Although quinpirole by itself had no effect on D1 receptors, co-administration with SKF-38393 attenuated the up-regulation of D1 receptors produced by SKF-38393 in the caudate-putamen and nucleus accumbens but not in the substantia nigra. The up-regulation of D1 receptors in response to chronic SKF-38393 may be attributed to the partial agonist properties of SKF-38393 which may not provide sufficient D1 receptor stimulation to down-regulate the receptor. Quinpirole-induced hypothermia and SKF-38393-induced hyperthermia were measured before and after chronic agonist treatments to examine the effects of these treatments on thermoregulatory functions mediated by each receptor subtype. Treatment with quinpirole or quinpirole plus SKF-38393 resulted in desensitization of quinpirole-induced hypothermia, whereas treatment with SKF-38393 alone had no effect. All of the chronic treatments produced sensitization of SKF-38393-induced hyperthermia. Since not all treatments result in an increase in the d. of D1 receptors, up-regulation of D1 receptors is not the sole mechanism for this sensitization. .