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)