2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. 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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GR 64349 acetate

GR 64349 acetate Chemical Structure

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GR 64349 acetate Related Antibodies

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Description

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[1][2].

IC50 & Target[1]

NK2R

 

In Vitro

GR 64349 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) 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 acetate Related Antibodies
In Vivo

Acetate of GR 64349 (0.1-10 nmoles/kg; intra-arterial injection) acts on peripheral NK-2 receptors to dose-dependently increase the tonic contraction level of the bladder and activate rhythmic bladder contractions in urethane-anesthetized rats, with an ED50 of 0.61 nmoles/kg i.a. for tonic contractions and an ED50 of 0.43 nmoles/kg i.a. for rhythmic bladder contractions[1].
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.

Animal Model: Wistar-Morini (male, 300-350 g, urethane-anesthetized, urinary bladder cannulated and filled to 0.25 mL saline)[1]
Dosage: 0.1 nmoles/kg; 1 nmoles/kg; 10 nmoles/kg
Administration: i.a.
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.
Molecular Weight

981.17

Formula

C44H72N10O13S
Sequence

Lys-Asp-Ser-Phe-Val-{Aaa}-Leu-Met-NH2
Sequence Shortening

KDSFV{Aaa}LM-NH2
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Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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GR 64349 acetate Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GR 64349GR64349GR-64349Neurokinin ReceptorNK receptorTachykinin receptorrat urinary bladder tissueneurokinin 2 (NK2) receptorNK-2 receptor subtypesmicturition reflexrat periaqueductal grey neuronsurethane-anesthetized ratsperipheral NK-2 receptorsInhibitorinhibitorinhibit

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