GR 64349 TFA
GR 64349 TFA is a selective neurokinin 2 (NK2) receptor agonist. GR 64349 TFA selectively activates the NK-2 receptor subtype. GR 64349 TFA activates tonic and rhythmic bladder contractions of the micturition reflex. GR 64349 TFA does not inhibit rhythmic bladder contraction activation induced by normal saline. GR 64349 TFA induces inward currents.
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- Fòrmula: C44H69F3N10O13S
- Peso molecular:1035.14
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Almacenamiento:
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
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NK2R |
GR 64349 TFA contracts isolated rat bladder tissues in vitro, with potency comparable to that of the selective NK-1 agonist GR 73632 (HY-P1192)[1].
GR 64349 (300-500 nM) TFA generates inward currents in some neurons[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GR 64349 (intracerebroventricular injection) TFA 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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Peso molecular 1035.14
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Fòrmula C44H69F3N10O13S
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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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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)
GR 64349 TFA Related Classifications
HY-P1278A Related Classifications
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