Delayed release formulation of the somatostatin analog RC-160 inhibits the growth hormone (GH) response to GH-releasing factor-(1-29)NH2 and decreases elevated prolactin levels in rats.
Bokser. L L; Schally. A V AV
Key Findings
- RC‑160 microcapsules released the drug at ~25 µg per day for a week.
- The drug blocked the GH surge caused by GRF‑(1‑29)NH2 for more than 96 hours.
- It also reduced elevated prolactin in female rats with pituitary grafts.
- Treated rats showed smaller weight gain compared with controls.
Practical Outcomes
- For biohackers interested in lowering GH or prolactin, this study suggests that a long‑acting somatostatin analog could be an effective tool, but the evidence is limited to rats and uses injectable microcapsules not available to the public. Until human safety and dosing data are available, the finding is mainly a proof‑of‑concept rather than a ready‑to‑use protocol.
Summary
In rats, a slow‑release injection of the somatostatin‑like drug RC‑160 kept growth‑hormone spikes down for at least four days after a growth‑hormone‑releasing signal and also lowered high prolactin levels. The treated rats gained less weight than untreated ones.
Abstract
Recently, we have developed a long-acting delivery system for our somatostatin (SS) analog RC-160 based on injectable microcapsules in poly-(D,L-lactide-coglycolide). We studied the capacity of this formulation to repeatedly block the GH secretion induced by administration of GRF-(1-29)NH2 (GRF) on different days. Male rats anesthetized with pentobarbital were injected iv with 2.5 micrograms/kg BW GRF-(1-29)NH2 or saline. Five minutes later, blood samples were taken for GH measurement, and the animals were injected im with RC-160 microcapsules at a dose calculated to release 25 micrograms/day of the analog for 7 days or with the vehicle. The GRF stimuli were repeated 48 h, 96 h, and 8 days after administration of SS analog in microcapsules. GRF administration increased GH levels at the four times tested (P less than 0.01) in the control group injected with vehicle, while RC-160 microcapsules inhibited the GH response for more than 96 h (P less than 0.01). The GH levels augmented by pentobarbital were also decreased by the RC-160 microcapsules (P less than 0.01). Animals treated with microcapsules showed smaller increases in their body weight than untreated rats (P less than 0.05). We also investigated the effect of RC-160 microcapsules on hyperprolactinemic female rats implanted with pituitary glands under the kidney capsules. High PRL levels in rats bearing pituitary grafts showed a significant decrease when measured 4 days after the administration of RC-160 microcapsules. These results demonstrate the efficacy of the long-acting delivery system of the SS analog RC-160 and suggest the possible clinical usefulness of this formulation for lowering GH and PRL levels.
Study Information
pubmed
1988
10.1210/endo-123-4-1735