Claims
- 1. A process of marking a 5HT.sub.2 -receptor with a radiolabeled compound comprising the steps of:
- (a) radiolabeling a compound of the formula: ##STR7## a pharmaceutically acceptable acid addition salt thereof or a stereoisomeric form thereof, wherein:
- R.sup.1 represents hydrogen or halo;
- R.sup.2 represents halo;
- R.sup.3 represents hydrogen or halo;
- --NR.sup.4 R.sup.5 represents azido; and
- Alk represents C.sub.2-4 alkanediyl,
- (b) administering said radiolabeled compound to biological material,
- (c) irradiating the receptor/marker complex with UV-light, and
- (d) detecting the emissions from the covalently bonded radiolabeled compound.
- 2. A process according to claim 1 wherein the compound is
- 4-amino-N-�1-�3-(4-fluorophenoxy)propyl!-4-methyl-4-piperidinyl!-5-iodo-2-methoxybenzamide;
- 4-amino-5-chloro-N-�1-�3-(4-fluorophenoxy)propyl!-4-methyl-4-piperidinyl!-2-methoxybenzamide;
- 4-amino-5-bromo-N-�1-�3-(4-fluorophenoxy)propyl!-4-methyl-4-piperidinyl-2-methoxybenzamide;
- 4-amino-N-�1-�3-(2-bromo-4-fluorophenoxy)propyl!-4-methyl-4-piperidinyl!-5-chloro-2-methoxybenzamide;
- 4-amino-N-�1-�3-(4-fluorophenoxy)propyl!-4-methyl-4-piperidinyl!-2-methoxybenzamide;
- 4-azido-5-chloro-N-�1-�3-(4-fluorophenoxy)propyl!-4-methyl-4-piperidinyl!-2-methoxybenzamide;
- 4-azido-N-�1-�3-(4-fluorophenoxy)propyl!-methyl-4-piperidinyl!-5-iodo-2-methoxybenzamide;
- 4-azido-5-bromo-N-�1-�3-(4-4-fluorophenoxy)propyl!-4-methyl-4-piperidinyl!-2-methoxybenzamide, or a pharmaceutically acceptable acid addition salt thereof.
- 3. A process according to claim 1 having at least one halo which is a radioactive isotope of iodine, bromine or fluorine.
- 4. A compound according to claim 1 wherein the compound is 4-amino-N-�1-�3-(4-fluorophenoxy)propyl!-4-methyl-4-piperidinyl!:5-iodo-2-methoxybenzamide, 5-.sup.125 I! or �5-.sup.123 I!.
CROSS-REFERENCE TO RELATED APPLICATIONS
This application is a division of application Ser. No. 08/367,111, filed on Jan. 6, 1995, now U.S. Pat. No. 5,498,618, which is a 371 of PCT/EP 93/01993, filed Jul. 8, 1993, published as WO94/02462, Feb. 3, 1994, which is a continuation of U.S. patent application Ser. No. 07/914,306, filed on Jul. 17, 1992 now abandoned.
Non-Patent Literature Citations (2)
Entry |
Azuma, C. "Marker reagents for detection of cell-surface receptors" CA 112:194927g, 1990. |
Gaudreau, P. "Fluorophore-linked growth hormone-releasing factor analog for marking receptors on pituitary cell surface and treatment of wounds, diorders or diseases": CA 125:2280, 1996. |
Divisions (1)
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367111 |
Jan 1995 |
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Continuations (1)
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914306 |
Jul 1992 |
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