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Chemical Compound Review:

CHEMBL114166 8-chloro-4-methyl-11-(3- methylbut-2-enoxy)...

Synonyms: AG-D-28602, SureCN8091302, ACMC-20mdr0, CHEBI:290658, C16H22ClNO, ...

Hieble, J.P. et al., Westby, J. et al., Medgett, I.C. et al., Daniel, E.E. et al., Kilpatrick, A.T. et al., et al.

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Disease relevance of Skf 104078

When infused during hypoxia, SKF 104078 decreased cardiac output and systemic blood pressure without affecting pulmonary pressure [1].

High impact information on Skf 104078

In competition with oxymetazoline, WB 4101, prazosin, ARC-239, SK&F 104078 and SK&F 104856, these rauwolscine binding sites were alpha 2A-like [2].
6-chloro-9-[(3-methyl-2-butenyl)oxy]-3-methyl-1H-2,3,4,5-tetrahydro-3- benzazepine (SK&F 104078) did not differentiate between the alpha-2A and alpha-2B receptor subtypes [3].
In contrast, SK&F 104078 competitively antagonized B-HT933 in the rat vas deferens (pA2 = 6.45) [4].
3. Yohimbine was approximately 10 times more potent postjunctionally than SK&F 104078 at antagonizing contractions to noradrenaline in human saphenous vein and at displacing [3H]-yohimbine binding in human platelet membranes [5].
The alpha 2-adrenoceptor antagonist SK&F 104078 has high affinity for 5-HT1A and 5-HT2 receptors [6].

Biological context of Skf 104078

Chloroethylclonidine pretreatment did not affect the ability of SK&F 104078 or SK&F 104856 to compete with rauwolscine binding sites on axonal membranes [2].
Characterization of alpha-adrenoceptors mediating sympathetic vasoconstriction in rat autoperfused hindlimb: effects of SK&F 104078 [7].
Intravenous (i.v.) administration of SK&F 104078 decreased blood pressure (BP) in both spontaneously hypertensive and DOCA-salt hypertensive rats [8].
The low oral bioavailability of SK&F 104078 did not appear to be due to high first-pass oxidative metabolism, since pretreatment of SHR with the suicide substrate inhibitor of cytochrome P-450, 1-aminobenzotriazole (ABT), did not result in increased oral efficacy [8].

Anatomical context of Skf 104078

The high affinity of SK&F 104078 for postjunctional alpha-2 adrenoceptors in the canine saphenous vein was confirmed by its ability to inhibit [3H]rauwolscine binding to postjunctional alpha-2 adrenoceptors in this tissue [9].
The results indicate that vascular neuroeffector transmission in rat hindlimb is mediated by postjunctional alpha 1-adrenoceptors, and that SK&F 104078 is a selective antagonist of postjunctional alpha 2-adrenoceptor, and lacks the prejunctional alpha 2-adrenoceptor antagonist action of rauwolscine [7].
These findings imply a negative inotropic effect of SK&F 104078 in metabolically vasodilated myocardium in the vicinity of an acute ischemic region [10].
Regional myocardial performance was measured by ultrasonic crystals in the anterior wall perfused by the left anterior descending coronary artery (LAD) before and during postjunctional alpha-adrenergic antagonism (SK&F 104078 2 mg/kg) [10].
Pretreatment of iris root/ciliary bodies with SKF 104078 or rauwolscine reversed the inhibitory effect of UK on isoproterenol- and VIP-induced accumulation of cAMP [11].

Associations of Skf 104078 with other chemical compounds

In the rat vas deferens, however, SK&F 104078 significantly antagonized the prejunctional alpha 2-adrenoceptor-mediated effects of clonidine and M-7 but did not block the responses to UK 14,304, xylazine, B-HT 933 and B-HT 920 [12].

Gene context of Skf 104078

SK&F 104078 had moderate affinity towards alpha 2-adrenoceptors (pKi 6.7) but displayed higher affinity at 5-HT1A (pKi 8.1) and 5-HT2 (pKi 7.6) receptors [6].

Analytical, diagnostic and therapeutic context of Skf 104078

Oral administration of SK&F 104078 had no significant effect on BP in SHR unless extremely high doses were administered [8].
SK&F 104078 did not alter regional myocardial shortening or the slope of end-systolic pressure-length relations in the control group [10].

References

Cardiovascular effects of SKF 104078 in lambs. Chappell, B., Padbury, J., Martinez, A., Habib, D., Stein, H., Oyama, K. Developmental pharmacology and therapeutics. (1991) [Pubmed]
Characterization of alpha 2 adrenoceptors and other adrenoceptors in membranes isolated from dog mesenteric nerve axons. Daniel, E.E., Gaspar, V., Berezin, I., Kwan, C.Y. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
Ability of SK&F 104078 and SK&F 104856 to identify alpha-2 adrenoceptor subtypes in NCB20 cells and guinea pig lung. Gleason, M.M., Hieble, J.P. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
Alpha 2-adrenoceptor blocking profile of SK&F 104078: further evidence for receptor subtypes. Akers, I., Coates, J., Drew, G.M., Sullivan, A.T. Br. J. Pharmacol. (1991) [Pubmed]
No evidence for differences between pre- and postjunctional alpha 2-adrenoceptors in the periphery. Connaughton, S., Docherty, J.R. Br. J. Pharmacol. (1990) [Pubmed]
The alpha 2-adrenoceptor antagonist SK&F 104078 has high affinity for 5-HT1A and 5-HT2 receptors. Kilpatrick, A.T., Brown, C.M., MacKinnon, A.C., Spedding, M. Eur. J. Pharmacol. (1989) [Pubmed]
Characterization of alpha-adrenoceptors mediating sympathetic vasoconstriction in rat autoperfused hindlimb: effects of SK&F 104078. Medgett, I.C., Ruffolo, R.R. Eur. J. Pharmacol. (1987) [Pubmed]
Cardiovascular effects of SK&F 104078, a novel alpha-adrenoceptor antagonist, in normotensive and hypertensive rats. Hieble, J.P., Sulpizio, A.C., Gutzait, L., Gombar, C.T. J. Cardiovasc. Pharmacol. (1990) [Pubmed]
Evidence for heterogeneity between pre- and postjunctional alpha-2 adrenoceptors using 9-substituted 3-benzazepines. Daly, R.N., Sulpizio, A.C., Levitt, B., DeMarinis, R.M., Regan, J.W., Ruffolo, R.R., Hieble, J.P. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
Postjunctional alpha-adrenergic stimulation of inotropy in hypoperfused myocardium outside an acute infarct. Westby, J., Birkeland, S., Hexeberg, E., Lekven, J., Grong, K. J. Cardiovasc. Pharmacol. (1992) [Pubmed]
Pharmacological evidence for heterogeneity of ocular alpha 2 adrenoceptors. Crosson, C.E., Heath, A.R., DeVries, G.W., Potter, D.E. Curr. Eye Res. (1992) [Pubmed]
Evidence for heterogeneity of prejunctional alpha-2-adrenoceptors. Oriowo, M.A., Hieble, J.P., Ruffolo, R.R. Pharmacology (1991) [Pubmed]

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