St 587
St 587 is a centrally acting α1-adrenoceptor agonist with an IC50 of 470 nM for rat α1-adrenoceptors. St 587 activates vascular postsynaptic α1-adrenoceptors, causing extracellular calcium influx-dependent vasoconstriction and pressor responses, and stimulates the hindlimb flexor reflex. St 587 can be used for research on neurological diseases.
For research use only. We do not sell to patients.
- CAS No.: 15327-37-4
- Formula: C10H9ClF3N3
- Molecular Weight:263.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
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- References
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Biological Activity
Description
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α1-adrenergic receptor 470 nM (IC50) |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
St 587 (1-30 μg; i.t.; single injection; 30 s) produces a dose-dependent spinal pressor response at 10 and 30 μg, but not at 1 μg[10].
St 587 (1-1000 µg/kg; i.v.; bolus administration) produces a dose-dependent pressor response in pithed normotensive rats, and this response is significantly attenuated by calcium channel blockade[6].
ST-587 (2 mL/kg; i.p.) produces hypothermic and sedative-like behavioral effects in healthy rats[5].
St 587 (0.5-30 μg; i.t.; single injection) produces hyperalgesia in the tail-flick and paw-pressure tests at low microgram doses[10].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male; 160-200 g)[1]
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Dosage:1 mg/kg
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Administration:i.v. (femoral vein)
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Result:Stimulated the hind limb flexor reflex in spinal rats at 1 mg/kg i.v.
Ipsapirone at 1 mg/kg i.v. reduced the stimulation in Fig. 10.
Ipsapirone at 3 mg/kg i.v. decreased the stimulation.
Ipsapirone at 35 mg/kg i.p. produced a total antagonistic effect.
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Animal Model:Sprague-Dawley (male, 350-450 g at experimentation)[10]
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Dosage:1, 10, and 30 μg
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Administration:i.t.; single injection; 30 sec
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Result:A slow and sustained rise in blood pressure and heart rate began 1 to 2 min after injection.
The 1-μg i.t. dose had no pressor effect.
The 10- and 30-μg i.t. doses produced a dose-dependent increase in mean arterial pressure.
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Animal Model:Sprague-Dawley (male, 350-450 g at experimentation)[10]
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Dosage:single i.t. injections of 0.5, 1.0, 3.0, and 30 μg; 1.0 or 30 μg 15 min after i.t. prazosin 2.5 μg
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Administration:i.t.; single injection; 15 min after i.t. prazosin in prior-prazosin groups
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Result:Mean baseline tail-flick latency was 2.63 sec and mean paw-pressure threshold was 206 g.
Tail-flick latency and paw-pressure threshold decreased below baseline across the 0.5-30 μg dose range.
Hyperalgesia was observed at 0.5, 1.0, and 3.0 μg.
At doses >3 μg, there was an apparent but incomplete return of tail-flick latency and paw-pressure threshold toward baseline.
Chemical Information
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CAS No. 15327-37-4
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Molecular Weight 263.65
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Formula C10H9ClF3N3
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SMILES
FC(F)(C1=CC=C(C(NC2=NCCN2)=C1)Cl)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Maj J, et al. Central action of ipsapirone, a new anxiolytic drug, on serotoninergic, noradrenergic and dopaminergic functions. Journal of neural transmission. 1987 Mar;70(1):1-7. [Content Brief]
[2]. Illes P, et al. Electrophysiological evidence for an alpha 2-adrenergic inhibitory control of transmitter release in the rabbit mesenteric artery. Eur J Pharmacol. 1987 Nov 10;143(2):151-61. [Content Brief]
[3]. Timmermans PB, et al. Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. J Med Chem. 1984 Apr;27(4):495-503. [Content Brief]
[4]. Puumala T, et al. Stimulation and blockade of α1 adrenoceptors affect behavioural activity, but not spatial working memory assessed by delayed non-matching to position task in rats. Journal of Psychopharmacology. 1997 Jan;11(1):45-51. [Content Brief]
[5]. Van der Laan JW, et al. The effects of centrally acting adrenergic agonists on temperature and on explorative and motor behaviour. Relation with effects on quasi-morphine withdrawal behaviour. European journal of pharmacology. 1985 Jan 08;107(3):367-73. [Content Brief]
[6]. Timmermans PB, et al. Differential effect of calcium entry blockers on alpha 1-adrenoceptor-mediated vasoconstriction in vivo. Naunyn Schmiedebergs Arch Pharmacol. 1983 Dec;324(4):239-45. [Content Brief]
[7]. Jonge AD, et al. A lipophilic, selective alpha1 -adrenoceptor agonist: 2-(2-chloro-5-trifluoromethylphenylimino)imida-zolidine (St 587). Life Sci. 1981 May 4;28(18):2009-16. [Content Brief]
[8]. Pussinen R, et al. Effects of D-cycloserine, a positive modulator of N-methyl-D-aspartate receptors, and ST 587, a putative alpha-1 adrenergic agonist, individually and in combination, on the non-delayed and delayed foraging behaviour of rats assessed in the radial arm maze. Journal of psychopharmacology (Oxford, England). 1999;13(2):171-9. [Content Brief]
[9]. Puumala T, et al. Effects of St-587 and prazosin on water maze and passive avoidance performance of scopolamine-treated rats. Pharmacology, biochemistry, and behavior. 1996 Sep;55(1):107-15. [Content Brief]
[10]. Loomis CW, et al. Intrathecal St-587: effects on nociceptive reflexes and blood pressure in the rat. The Journal of pharmacology and experimental therapeutics. 1992 Nov;263(2):428-35. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
St 587 Related Classifications
HY-189058 Related Classifications
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