US4801575A
Expired / Lapsed
US
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Chimeric peptides for neuropeptide delivery through the blood-brain barrier
Assignee: University of California Berkeley
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Filing: 1986-07-30
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Granted: 1989-01-31
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Expires: 2006-07-30
Abstract
Abstract Chimeric peptides adapted for delivering neuropharmaceutical agents, such as neuropeptides into the brain by receptor-mediated transcytosis through the blood-brain barrier. The chimeric peptides include a peptide which by itself is capable of crossing the blood-brain barrier by transcytosis at a relatively high rate. The transportable peptide is conjugated to a hydrophilic neuropeptide which by itself is transportable only at a very low rate into the brain across the blood-brain barrier. The resulting chimeric peptide is transported into the brain at a much higher rate than the neuropeptide alone to thereby provide an effective means for introducing hydrophilic neuropeptides into the brain through the blood-brain barrier.
Inventors
- 👤 William M. Pardridge
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 18:01
CPC Classifications
C; C07; C07K; C07K1/00; C07K1/107; C07K1/1072; C07K1/1075; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/62; C07K14/00; C07K14/435; C07K14/575; C07K14/62; C07K14/655; C07K14/665; C07K14/675; C07K14/695; C07K7/00; C07K7/04; C07K7/16; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/15; Y10S930/16; Y10S930/26
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
82 words
A chimeric peptide adapted for delivering a neuropharmaceutical agent into the brain by transcytosis through the blood-brain barrier, said chimeric peptide comprising: a transportable peptide capable of crossing the blood-brain barrier by transcytosis, said peptide being selected from the group consisting of insulin, transferrin, IGF-I, IGF-II, basic albumin and prolactin; and a neuropharmaceutical agent selected from the group consisting of somatostatin, thyrotropin releasing hormone, vasopressin, alpha interferon, endorphin, muramyl dipeptide and L-methionyl(sulfone)-L-glutamyl-L-histidyl-L-phenylalanyl-D-lysyl-L-phenylalanine, wherein said neuropharmaceutical agent is conjugated with said transportable peptide.
Claim 2
Dependent Claim
82 words
A chimeric peptide adapted for delivering a neuropharmaceutical agent into the brain by transcytosis through the blood-brain barrier, said chimeric peptide comprising: a transportable peptide capable of crossing the blood-brain barrier by transcytosis, said peptide being selected from the group consisting of insulin, transferrin, IGF-I, IGF-II, basic albumin and prolactin; and a neuropharmaceutical agent selected from the group consisting of somatostatin, thyrotropin releasing hormone, vasopressin, alpha interferon, endorphin, muramyl dipeptide and L-methionyl(sulfone)-L-glutamyl-L-histidyl-L-phenylalanyl-D-lysyl-L-phenylalanine, wherein said neuropharmaceutical agent is conjugated with said transportable peptide.
Claim 3
Dependent Claim
20 words
A chimeric peptide according to claim 1 wherein said transportable peptide and neuropharmaceutical agent are conjugated via a conjugation agent.
Claim 4
Dependent Claim
30 words
A chimeric peptide according to claim 2 wherein said conjugation agent is capable of conjugating the transportable peptide to said neuropharmaceutical agent by peptide thiolation or lysine coupling via glutaraldehyde.
Claim 5
Dependent Claim
13 words
A chimeric peptide according to claim 3 wherein said transportable peptide is insulin.
Claim 6
Dependent Claim
13 words
A chimeric peptide according to claim 4 wherein said neuropharmaceutical agent is somatostatin.
Claim 7
Dependent Claim
23 words
A chimeric peptide according to claim 1 having the formula ##STR3## wherein A is said neuropharmaceutical agent and B is said transportable peptide.
Claim 8
Dependent Claim
15 words
A chimeric peptide according to claim 6 wherein A is somatostatin and B is insulin.
Claim 9
Dependent Claim
19 words
A composition comprising a chimeric peptide according to claim 1 and a pharmaceutically acceptable carrier for said chimeric peptide.
Claim 10
Dependent Claim
14 words
A composition according to claim 8 wherein said pharmaceutically acceptable carrier is sterile saline.
Claim 11
Independent Claim
67 words
A method for delivering a neuropharmaceutical agent into the brain of an animal by transcytosis through the blood-brain barrier comprising the step of introducing a chimeric peptide into the bloodstream of said animal in a sufficient amount to provide transport of said chimeric peptide across said blood-brain barrier, wherein said chimeric peptide comprises a transportable peptide capable of crossing the blood-brain barrier conjugated with a neuropharmaceutical agent.
Claim 12
Independent Claim
67 words
A method for delivering a neuropharmaceutical agent into the brain of an animal by transcytosis through the blood-brain barrier comprising the step of introducing a chimeric peptide into the bloodstream of said animal in a sufficient amount to provide transport of said chimeric peptide across said blood-brain barrier, wherein said chimeric peptide comprises a transportable peptide capable of crossing the blood-brain barrier conjugated with a neuropharmaceutical agent.
Claim 13
Dependent Claim
17 words
A method according to claim 10 wherein said chimeric peptide is introduced intra into the subject's bloodstream.
Claim 14
Dependent Claim
48 words
In a method for introducing a neuropharmaceutical agent into the brain across the blood-brain barrier, wherein the improvement comprises increasing the rate at which said neuropharmaceutical agent crosses the blood-brain barrier by conjugating said neuropharmaceutical agent with a transportable peptide capable of crossing the blood-brain carrier by transcytosis.
Claim 15
Dependent Claim
48 words
In a method for introducing a neuropharmaceutical agent into the brain across the blood-brain barrier, wherein the improvement comprises increasing the rate at which said neuropharmaceutical agent crosses the blood-brain barrier by conjugating said neuropharmaceutical agent with a transportable peptide capable of crossing the blood-brain carrier by transcytosis.
Claim 16
Dependent Claim
25 words
A method according to claim 10 wherein said transportable peptide is selected from the group consisting of insulin, transferrin, IGF-I, IGF-II, basic albumin and prolactin.
Claim 17
Dependent Claim
14 words
A method according to claim 10 wherein said neuropharmaceutical agent is a hydrophilic peptide.
Claim 18
Dependent Claim
29 words
A method according to claim 14 wherein said neuropharmaceutical agent is selected from the group consisting of somatostatin, thyrotropin releasing hormone, vasopressin, alpha interferon, endorphin, muramyl dipeptide and L-methionyl(sulfone)-L-glutamyl-L-histidyl-L-phenylalanyl-D-lysyl-L-phenylalanine.
Claim 19
Dependent Claim
19 words
A method according to claim 10 wherein said transportable peptide and neuropharmaceutical agent are conjugated via a conjugation agent.
Claim 20
Dependent Claim
29 words
A method according to claim 16 wherein said conjugation agent is capable of conjugating the transportable peptide to said neuropharmaceutical agent by peptide thiolation or lysine coupling via glutaraldehyde.
Claim 21
Dependent Claim
12 words
A method according to claim 17 wherein said transportable peptide is insulin.
Claim 22
Dependent Claim
12 words
A method according to claim 18 wherein said neuropharmaceutical agent is somatostatin.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1992-01-31 | 1992-08-01 | 1993-01-31 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-01-31 | 1996-08-01 | 1997-01-31 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-01-31 | 2000-08-01 | 2001-01-31 | $7700.00 | Window Closed / Lapsed |