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Page 1
Ability of SK&F 104078 and SK&F 104856 to identify alpha-2 adrenoceptor subtypes in NCB20 cells and guinea pig lung.
Gleason MM, Hieble JP. Gleason MM, et al. J Pharmacol Exp Ther. 1991 Dec;259(3):1124-32. J Pharmacol Exp Ther. 1991. PMID: 1684814
However, 2-vinyl-7-chloro-3,4,5,6-tetrahydro-4-methylthieno[(4,3,2ef] [3]benzazepine (SK&F 104856), which has similar selectivity in functional in vitro models, was about 35-fold more potent in displacing [3H]rauwolscine binding to the alpha-2B site. Thes …
However, 2-vinyl-7-chloro-3,4,5,6-tetrahydro-4-methylthieno[(4,3,2ef] [3]benzazepine (SK&F 104856), which has simil …
Cardiovascular actions of a new selective postjunctional alpha-adrenoceptor antagonist, SK&F 104856, in normotensive and hypertensive dogs.
Hieble JP, Nichols AJ, Fredrickson TA, DePalma PD, Ruffolo RR Jr, Brooks DP. Hieble JP, et al. Br J Pharmacol. 1992 Apr;105(4):992-6. doi: 10.1111/j.1476-5381.1992.tb09090.x. Br J Pharmacol. 1992. PMID: 1354539 Free PMC article.
SK&F 104856 as well as prazosin and SK&F 86466 reduced blood pressure in the anaesthetized normotensive dog. 3. SK&F 86466 and rauwolscine but not SK&F 104856 or prazosin, produced a marked incr …
SK&F 104856 as well as prazosin and SK&F 86466 reduced blood pressure in the anaesthetized normot …
Additional evidence for functional subclassification of alpha-2 adrenoceptors based on a new selective antagonist, SK&F 104856.
Hieble JP, Sulpizio AC, Edwards R, Chapman H, Young P, Roberts SP, Blackburn TP, Wood MD, Shah DH, Demarinis RM, et al. Hieble JP, et al. J Pharmacol Exp Ther. 1991 Nov;259(2):643-52. J Pharmacol Exp Ther. 1991. PMID: 1682482
SK&F 104856 is more potent than SK&F 104078, and lacks the 5-hydroxytryptamine receptor antagonist activity associated with the earlier compound. ...The results obtained with SK&F 104856 provide additional eviden …
SK&F 104856 is more potent than SK&F 104078, and lacks the 5-hydroxytryptamine receptor antagonis …
The prejunctional inhibitory effect of alpha-methylnoradrenaline in the rat vas deferens is not mediated via alpha 2-adrenoceptors.
Oriowo MA. Oriowo MA. J Pharm Pharmacol. 1995 Aug;47(8):661-4. doi: 10.1111/j.2042-7158.1995.tb05855.x. J Pharm Pharmacol. 1995. PMID: 8583368
The inhibitory effect of alpha-methylnoradrenaline was also not antagonized by phentolamine (3 x 10(-7) M), SK&F 104856 (2-vinyl-7-chloro-3,4,5,6-tetrahydro-4-methylthienol[4,3,2 ef][3]benzazepine) 3 x 10(-6) M) or yohimbine 3 x 10(-7) M). ...The -logKB v …
The inhibitory effect of alpha-methylnoradrenaline was also not antagonized by phentolamine (3 x 10(-7) M), SK&F 104856 …
Characterization of alpha 2 adrenoceptors and other adrenoceptors in membranes isolated from dog mesenteric nerve axons.
Daniel EE, Gaspar V, Berezin I, Kwan CY. Daniel EE, et al. J Pharmacol Exp Ther. 1995 Nov;275(2):978-86. J Pharmacol Exp Ther. 1995. PMID: 7473191
In competition with oxymetazoline, WB 4101, prazosin, ARC-239, SK&F 104078 and SK&F 104856, these rauwolscine binding sites were alpha 2A-like. Chloroethylclonidine pretreatment did not affect the ability of SK&F 104078 …
In competition with oxymetazoline, WB 4101, prazosin, ARC-239, SK&F 104078 and SK&F 104856, these …
Different alpha-adrenoceptor subtypes mediate constriction of arterioles and venules.
Leech CJ, Faber JE. Leech CJ, et al. Am J Physiol. 1996 Feb;270(2 Pt 2):H710-22. doi: 10.1152/ajpheart.1996.270.2.H710. Am J Physiol. 1996. PMID: 8779849

Venule sensitivity to UK-14,304 was reduced fivefold by BRL-44408 (P < 0.05), whereas ARC-239 had no effect. alpha 2 Subtype-selective antagonists inhibited UK-14,304 constriction of venules, with 50% inhibitory concentration values for BRL-44408 (alpha 2D-selective) of 6.04 +

…

Venule sensitivity to UK-14,304 was reduced fivefold by BRL-44408 (P < 0.05), whereas ARC-239 had no effect. alpha 2 Subtype-selective an

…
Peripheral nociceptive effects of alpha 2-adrenergic receptor agonists in the rat.
Khasar SG, Green PG, Chou B, Levine JD. Khasar SG, et al. Neuroscience. 1995 May;66(2):427-32. doi: 10.1016/0306-4522(94)00562-j. Neuroscience. 1995. PMID: 7477883
Norepinephrine (100 ng) hyperalgesia was dose-dependently antagonized by alpha 2-adrenergic receptor antagonists. From the estimated ID50, the rank order of potency was: SK&F 104856 (alpha 2B) approximately imiloxan (alpha 2B) > rauwolscine (alpha 2C) …
Norepinephrine (100 ng) hyperalgesia was dose-dependently antagonized by alpha 2-adrenergic receptor antagonists. From the estimated ID50, t …
Infusions of alpha-2 noradrenergic agonists and antagonists into the amygdala: effects on kindling.
Pelletier MR, Corcoran ME. Pelletier MR, et al. Brain Res. 1993 Dec 31;632(1-2):29-35. doi: 10.1016/0006-8993(93)91134-e. Brain Res. 1993. PMID: 7908598
Unexpectedly, intraamygdaloid infusions of the alpha-2 antagonists idazoxan, yohimbine, and SK&F 104856 failed to accelerate kindling. Infusion of the alpha-1 antagonist corynanthine also failed to affect kindling. ...
Unexpectedly, intraamygdaloid infusions of the alpha-2 antagonists idazoxan, yohimbine, and SK&F 104856 failed to a …
Alpha 2-adrenoceptor antagonists potentiate acetylcholinesterase inhibitor effects on passive avoidance learning in the rat.
Camacho F, Smith CP, Vargas HM, Winslow JT. Camacho F, et al. Psychopharmacology (Berl). 1996 Apr;124(4):347-54. doi: 10.1007/BF02247440. Psychopharmacology (Berl). 1996. PMID: 8739550
This synergistic interaction may represent effects of antagonism of presynaptic alpha 2-adrenoceptor since coadministration of heptylphysostigmine and the selective postsynaptic alpha 2-adrenoceptor antagonist SKF 104856 did not result in enhanced learning. Taken to …
This synergistic interaction may represent effects of antagonism of presynaptic alpha 2-adrenoceptor since coadministration of heptylphysost …
Characterization of alpha-adrenoceptor activity in term-newborn piglet mesentery.
Ferrara JJ, Hoang TV, Choe EU, Lippton HL, Hyman AL, Flint LM. Ferrara JJ, et al. J Pharm Pharmacol. 1996 Dec;48(12):1298-301. doi: 10.1111/j.2042-7158.1996.tb03939.x. J Pharm Pharmacol. 1996. PMID: 9004194
That the mesenteric vasoconstrictor response to mesenteric plexus stimulation was unaltered by CEC, but was muted by both WB 4101 and SK&F 104856 (a post-junctional alpha 1- and alpha 2-adrenoceptor antagonist) suggests that pre- and post-junctional alpha …
That the mesenteric vasoconstrictor response to mesenteric plexus stimulation was unaltered by CEC, but was muted by both WB 4101 and SK …