US5232684A
Expired / Lapsed
US
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Labelled resiniferatoxin, compositions thereof, and methods for using the same
Assignee: United States Department of Health and Human Services
•
Filing: 1990-06-29
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Granted: 1993-08-03
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Expires: 2010-06-29
Abstract
Abstract The present invention relates to labelled resiniferatoxin and congeners thereof. Preferably, the labelled compounds of the invention are radio or fluorescently labelled. The invention is further directed to compositions comprising these labelled compounds, as well as to methods of using these compounds.
Inventors
- 👤 Peter M. Blumberg
- 👤 Arpad Szallasi
- 👤 Zoltan Szallasi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 14:02
CPC Classifications
A; A61; A61K; A61K49/00; A61K49/001; A61K49/0013; A61K49/0017; A61K49/0019; A61K49/0021; A61K49/005; A61K49/0052; A61K51/00; A61K51/02; A61K51/04; A61K51/08; C; C07; C07D; C07D493/00; C07D493/12; C07D493/18; G; G01; G01N; G01N33/00; G01N33/48; G01N33/50; G01N33/53; G01N33/531; G01N33/532; G01N33/534; A61K2123/00
Claims Analysis
Total Claims: 50
Claim 1
Independent Claim
8 words
An isolated compound consisting essentially of radiolabelled resiniferatoxin.
Claim 2
Dependent Claim
8 words
An isolated compound consisting essentially of radiolabelled resiniferatoxin.
Claim 3
Dependent Claim
24 words
The isolated labelled resiniferatoxin of claim 1, wherein the label is selected from the group consisting of a tritium label and an iodine label.
Claim 4
Dependent Claim
18 words
The compound selected from the group consisting of tritium labelled resiniferatoxin, I-131 labelled resiniferatoxin and I-125 labelled resiniferatoxin.
Claim 5
Dependent Claim
18 words
The compound selected from the group consisting of tritium labelled resiniferatoxin, I-131 labelled resiniferatoxin and I-125 labelled resiniferatoxin.
Claim 6
Dependent Claim
3 words
Isolated labelled resiniferatoxin.
Claim 7
Dependent Claim
3 words
Isolated labelled resiniferatoxin.
Claim 8
Dependent Claim
49 words
The compound of claim 4 wherein said resiniferatoxin or congeners thereof having the formula: ##STR17## where ##STR18## R 3 is OH, X is 0 or 1, R 1 , R 2 , R 4 and R 5 each are: H, OH ##STR19## with n=0 to 10 are fluorescently labeled.
Claim 9
Dependent Claim
27 words
The compound of claim 5, wherein the fluorescent labels are selected from the group consisting of fluorescein, rhodamine, eosin, erythrosin, pyrene, anthracene, acridine, dimethylaminophytyl and 7-nitrobenzo-2-oxa-1,3-diazole (NBD).
Claim 10
Dependent Claim
5 words
Tritium or iodine radiolabelled resiniferatoxin.
Claim 11
Dependent Claim
5 words
Tritium or iodine radiolabelled resiniferatoxin.
Claim 12
Dependent Claim
65 words
A labelled compound having the formula: ##STR20## where ##STR21## R 3 is OH, X is 0 or 1, R 1 , R 2 , R 4 and R 5 each are: H, OH, ##STR22## with n=0 to 10. wherein at least one of R 1 , R 2 , R 4 , or R 5 is labelled with 3 H, 125 I or 131 I.
Claim 13
Dependent Claim
65 words
A labelled compound having the formula: ##STR20## where ##STR21## R 3 is OH, X is 0 or 1, R 1 , R 2 , R 4 and R 5 each are: H, OH, ##STR22## with n=0 to 10. wherein at least one of R 1 , R 2 , R 4 , or R 5 is labelled with 3 H, 125 I or 131 I.
Claim 14
Dependent Claim
40 words
Isolated radiolabelled congeners of resiniferatoxin having the formula: ##STR23## where ##STR24## R 3 is OH, X is 0 or 1, R 1 , R 2 , R 4 and R 5 each are: H, OH, ##STR25## with n=0 to 10
Claim 15
Dependent Claim
40 words
Isolated radiolabelled congeners of resiniferatoxin having the formula: ##STR23## where ##STR24## R 3 is OH, X is 0 or 1, R 1 , R 2 , R 4 and R 5 each are: H, OH, ##STR25## with n=0 to 10
Claim 16
Dependent Claim
56 words
Radiolabelled congeners of resiniferatoxin having the formula: ##STR26## where ##STR27## R 3 is OH, X is 0 or 1, R 1 , R 2 , R 4 and R 5 each are: H, OH, ##STR28## with n=0 to 10, wherein the label is selected from the group consisting of a tritium label and an iodine label.
Claim 17
Dependent Claim
56 words
Radiolabelled congeners of resiniferatoxin having the formula: ##STR26## where ##STR27## R 3 is OH, X is 0 or 1, R 1 , R 2 , R 4 and R 5 each are: H, OH, ##STR28## with n=0 to 10, wherein the label is selected from the group consisting of a tritium label and an iodine label.
Claim 18
Dependent Claim
62 words
The compound having the formula: ##STR29## where ##STR30## R 3 is OH, X is 0 or 1, R 1 , R 2 , R 4 and R 5 each are: H, OH, ##STR31## with n=0 to 10, and at least one R 1 , R 2 , R 4 or R 5 is labelled with 3 H, 125 I or 131 I.
Claim 19
Dependent Claim
62 words
The compound having the formula: ##STR29## where ##STR30## R 3 is OH, X is 0 or 1, R 1 , R 2 , R 4 and R 5 each are: H, OH, ##STR31## with n=0 to 10, and at least one R 1 , R 2 , R 4 or R 5 is labelled with 3 H, 125 I or 131 I.
Claim 20
Dependent Claim
24 words
The compound of claim 11, wherein said congener has the formula: ##STR32## wherein R' is a fluorescent label and n is 0 to 10.
Claim 21
Dependent Claim
3 words
Isolated radiolabelled tinyatoxin.
Claim 22
Dependent Claim
3 words
Isolated radiolabelled tinyatoxin.
Claim 23
Dependent Claim
6 words
The compound having the formula ##STR33##
Claim 24
Dependent Claim
6 words
The compound having the formula ##STR33##
Claim 25
Dependent Claim
10 words
The compound having the formula ##STR34## where X is 1--3.
Claim 26
Dependent Claim
10 words
The compound having the formula ##STR34## where X is 1--3.
Claim 27
Dependent Claim
11 words
The compound of claim 15, wherein X is 1 or 2.
Claim 28
Dependent Claim
6 words
The compound having the formula ##STR35##
Claim 29
Dependent Claim
6 words
The compound having the formula ##STR35##
Claim 30
Dependent Claim
6 words
The compound having the formula ##STR36##
Claim 31
Dependent Claim
6 words
The compound having the formula ##STR36##
Claim 32
Dependent Claim
6 words
The compound having the formula ##STR37##
Claim 33
Dependent Claim
6 words
The compound having the formula ##STR37##
Claim 34
Dependent Claim
6 words
The compound having the formula ##STR38##
Claim 35
Dependent Claim
6 words
The compound having the formula ##STR38##
Claim 36
Dependent Claim
10 words
The compound having the formula ##STR39## where X is 1-3.
Claim 37
Dependent Claim
10 words
The compound having the formula ##STR39## where X is 1-3.
Claim 38
Dependent Claim
11 words
The compound of claim 21, wherein X is 1 or 2.
Claim 39
Dependent Claim
6 words
The compound having the formula ##STR40##
Claim 40
Dependent Claim
6 words
The compound having the formula ##STR40##
Claim 41
Dependent Claim
7 words
The compound having the formula ##STR41## 25.
Claim 42
Dependent Claim
7 words
The compound having the formula ##STR41## 25.
Claim 43
Dependent Claim
6 words
The compound having the formula ##STR42##
Claim 44
Dependent Claim
6 words
The compound having the formula ##STR42##
Claim 45
Dependent Claim
6 words
The compound having the formula ##STR43##
Claim 46
Dependent Claim
6 words
The compound having the formula ##STR43##
Claim 47
Dependent Claim
21 words
A composition comprising an effective amount of the compound of claim 1 for use in receptor binding and a suitable carrier.
Claim 48
Dependent Claim
21 words
A composition comprising an effective amount of the compound of claim 3 for use in receptor binding and a suitable carrier.
Claim 49
Dependent Claim
21 words
A composition comprising an effective amount of the compound of claim 5 for use in receptor binding and a suitable carrier.
Claim 50
Dependent Claim
33 words
A method for detecting a capsaicin receptor in a subject, which comprises administering to a subject the labelled compound of claim 1, and measuring the amount of said labelled compound in said subject.
References Cited (Backward Citations)
US4939149A
Cited
US5021450A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1996-08-02 | 1997-02-01 | 1997-08-03 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-08-02 | 2001-02-01 | 2001-08-03 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-08-02 | 2005-02-01 | 2005-08-03 | $7700.00 | Window Closed / Lapsed |