Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C26H21FN2O3 |
| Molecular Weight | 428.4549 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H](N(CC1=CC(=CC=C1)C(O)=O)C(=O)C2=CC3=CC=CC=C3N=C2)C4=CC=C(F)C=C4
InChI
InChIKey=BXNMZRPTQFVRFA-QGZVFWFLSA-N
InChI=1S/C26H21FN2O3/c1-17(19-9-11-23(27)12-10-19)29(16-18-5-4-7-21(13-18)26(31)32)25(30)22-14-20-6-2-3-8-24(20)28-15-22/h2-15,17H,16H2,1H3,(H,31,32)/t17-/m1/s1
| Molecular Formula | C26H21FN2O3 |
| Molecular Weight | 428.4549 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 12:01:45 GMT 2023
by
admin
on
Sat Dec 16 12:01:45 GMT 2023
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| Record UNII |
F2B10OFV7Y
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| Record Status |
Validated (UNII)
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| Record Version |
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Common Name | English | ||
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1398583-31-7
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DTXSID301336742
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DB15450
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F2B10OFV7Y
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60195662
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PF-05105679
Created by
admin on Sat Dec 16 12:01:45 GMT 2023 , Edited by admin on Sat Dec 16 12:01:45 GMT 2023
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PRIMARY | Description: TRPM8 inhibitor (IC50 value 0.1 .MU.M for TRPM8 in single cell patch clamp electrophysiology (Ephys) studies), showing >100-fold selectivity across a range of different receptors, ion channels, and enzymes including the closely related TRPV1 and TRPA1 channels. Although PF-05105679 shows no effect on core body temperature in humans, it proofs to be a useful tool to study in vitro effects of TRPM8 on thermoregulation and for the treatment of pain in humans. | ||
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PF-05105679
Created by
admin on Sat Dec 16 12:01:45 GMT 2023 , Edited by admin on Sat Dec 16 12:01:45 GMT 2023
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
The transient receptor potential (TRP) family of ion channels comprises nonselective cation channels that respond to a wide range of chemical and thermal stimuli. TRPM8, a member of the melastatin subfamily, is activated by cold temperatures (<28 C), and antagonists of this channel have the potential to treat cold induced allodynia and hyperalgesia. However, TRPM8 has also been implicated in mammalian thermoregulation and antagonists have the potential to induce hypothermia in patients. We report herein the identification and optimization of a series of TRPM8 antagonists that ultimately led to the discovery of PF-05105679. The clinical finding with this compound will be discussed, including both efficacy and its ability to affect thermoregulation processes in humans.
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ACTIVE MOIETY |
Originator: Pfizer; Class: Analgesic; Mechanism of Action: TRPM8 protein inhibitor; Orphan Drug Status: No; On Fast track: No; New Molecular Entity: Yes; Highest Development Phase: No development reported for Pain; Most Recent Events: 30 Sep 2011 Pfizer completes a phase I trial in Healthy volunteers in Belgium (NCT01393652), 23 May 2011 Phase-I clinical trials in Pain in Belgium (unspecified route)
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ACTIVE MOIETY |
Official Title: A Phase I, Randomized, Placebo-Controlled, Dose Escalating Cross Over Study To Evaluate The Safety, Toleration, Pharmacokinetics And Pharmacodynamics Of PF-05105679 Under Fasted Conditions In Healthy Volunteers
Purpose: This is a two part study. The purpose of the first part (Part A) is the evaluation of the pharmacokinetics, safety and tolerability after single ascending dose of PF-05105679. The second part (Part B) of this study will focus on the exploratory pharmacodynamics of PF-05105679 using pharmacodynamics markers (cold detection) in healthy volunteers. The doses selected in Part B will have been administered previously in the Part A of the study.
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ACTIVE MOIETY |
Drugs: Oxycodone, PF 5105679; Indication: Pain; Focus: Adverse reactions, Pharmacodynamics, Pharmacokinetics; Acronyms: SINGLE DOSE; Most Recent Events: 30 Sep 2011 Status changed from recruiting to completed as reported by ClinicalTrials.gov., 15 Jul 2011 New trial record
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