FR 113680
FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor.
For research use only. We do not sell to patients.
- CAS No.: 126088-92-4
- Formula: C35H39N5O6
- Molecular Weight:625.71
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
The inhibitory effect of FR 113680 on SP-induced guinea-pig ileum contraction is competitive and the pA2 value is 7.53[1].
FR 113680 has not effect on [3H]-SP binding to rat cerebral cortical membranes (NK1), [3H]-neurokinin A ([3H]-NKA) binding to rat duodenum smooth muscle membranes (NK2) and [3H]-eledoisin (Ele) binding to rat cerebral cortical membranes (NK3)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats, cigarette smoke-induced rat tracheal plasma extravasation model[2]
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Dosage:0, 10 and 32 mg/kg
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Administration:IV, once
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Result:Significantly inhibited cigarette smoke-induced rat tracheal plasma extravasation at a dose of 32 mg/kg.
Chemical Information
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CAS No. 126088-92-4
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Molecular Weight 625.71
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Formula C35H39N5O6
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Sequence
Ac-Thr-{d-Trp(For)}-{Phe(NMe,Bzl)}
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Sequence Shortening
Ac-T-{d-Trp(For)}-{Phe(NMe,Bzl)}
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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]. Morimoto H, et al. FR 113680: a novel tripeptide substance P antagonist with NK1 receptor selectivity. Br J Pharmacol. 1992 May;106(1):123-6. [Content Brief]
[2]. Morimoto H, et al. Effects of FR 113680 and FK 224, novel tachykinin receptor antagonists, on cigarette smoke-induced rat tracheal plasma extravasation. Eur J Pharmacol. 1992 Nov 24;224(1):1-5. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)