GR 64349 acetate
GR 64349 acetate is a selective neurokinin 2 (NK2) receptor agonist. GR 64349 acetate selectively activates the NK-2 receptor subtype. GR 64349 acetate activates tonic and rhythmic bladder contractions of the micturition reflex. GR 64349 acetate does not inhibit rhythmic bladder contraction activation induced by normal saline. GR 64349 acetate induces inward currents.
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- 화학식: C44H72N10O13S
- 분자량:981.17
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
NK2R |
In Vitro
GR 64349 acetate contracts isolated rat bladder tissues in vitro, with potency comparable to that of the selective NK-1 agonist GR 73632[1].
GR 64349 (300-500 nM) acetate generates inward currents in some neurons[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GR 64349 (intracerebroventricular injection) acetate does not modulate centrally mediated rhythmic bladder contractions in urethane-anesthetized rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar-Morini (male, 300-350 g, urethane-anesthetized, urinary bladder cannulated and filled to 0.25 mL saline)[1]
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Dosage:0.1 nmoles/kg; 1 nmoles/kg; 10 nmoles/kg
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Administration:i.a.
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Result:Induced a dose-related increase in intravesical pressure (tonic contraction, TC) and activation of rhythmic bladder contractions (RBC).
Reached maximal TC amplitude of 37 mmHg (n=6-7).
Achieved ED50 of 0.61 nmoles/kg i.a. for TC (95% confidence limits: 0.36-1.03).
Achieved ED50 of 0.43 nmoles/kg i.a. for RBC (95% confidence limits: 0.15-1.26).
Observed RBC in 4-6 out of 6 preparations at 1 nmoles/kg i.a.
Left TC largely unaffected after topical TTX pretreatment, which abolished RBC.
Showed maximal TC amplitudes of 28 mmHg (without antagonist) and 26 mmHg (with GR 82334 pretreatment, n=5), with GR 82334 not inhibiting GR 64349-induced TC.
Chemical Information
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분자량 981.17
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화학식 C44H72N10O13S
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Sequence
Lys-Asp-Ser-Phe-Val-{Aaa}-Leu-Met-NH2
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Sequence Shortening
KDSFV{Aaa}LM-NH2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Palea S, et al. Further studies on the effects of selective neurokinin agonists upon the activation of micturition reflex in rats. Evidence for a dual NK-1 receptor mediated excitatory and inhibitory activity. Neuropeptides. 1993 May;24(5):285-91. [Content Brief]
[2]. Drew GM, et al. Postsynaptic actions of substance P on rat periaqueductal grey neurons in vitro. Neuropharmacology. 2005;49(5):587-595. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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